Non-depolarizing Neuromuscular Blocking Activity of Bisquaternary Amino Di- and Tripeptide Derivatives (Englisch)
- Neue Suche nach: Booij, L. H. D. J.
- Neue Suche nach: van der Broek, L. A. G. M.
- Neue Suche nach: Caulfield, W.
- Neue Suche nach: Dommerholt-Caris, B. M. G.
- Neue Suche nach: Clark, J. K.
- Neue Suche nach: van Egmond, J.
- Neue Suche nach: McGuire, R.
- Neue Suche nach: Muir, A. W.
- Neue Suche nach: Ottenheijm, H. C. J.
- Neue Suche nach: Rees, D. C.
- Neue Suche nach: Booij, L. H. D. J.
- Neue Suche nach: van der Broek, L. A. G. M.
- Neue Suche nach: Caulfield, W.
- Neue Suche nach: Dommerholt-Caris, B. M. G.
- Neue Suche nach: Clark, J. K.
- Neue Suche nach: van Egmond, J.
- Neue Suche nach: McGuire, R.
- Neue Suche nach: Muir, A. W.
- Neue Suche nach: Ottenheijm, H. C. J.
- Neue Suche nach: Rees, D. C.
In:
JOURNAL OF MEDICINAL CHEMISTRY
;
43
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4822-4833
;
2000
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ISSN:
- Aufsatz (Zeitschrift) / Print
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Titel:Non-depolarizing Neuromuscular Blocking Activity of Bisquaternary Amino Di- and Tripeptide Derivatives
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Beteiligte:Booij, L. H. D. J. ( Autor:in ) / van der Broek, L. A. G. M. ( Autor:in ) / Caulfield, W. ( Autor:in ) / Dommerholt-Caris, B. M. G. ( Autor:in ) / Clark, J. K. ( Autor:in ) / van Egmond, J. ( Autor:in ) / McGuire, R. ( Autor:in ) / Muir, A. W. ( Autor:in ) / Ottenheijm, H. C. J. ( Autor:in ) / Rees, D. C. ( Autor:in )
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Erschienen in:JOURNAL OF MEDICINAL CHEMISTRY ; 43 ; 4822-4833
-
Verlag:
- Neue Suche nach: ACS AMERICAN CHEMICAL SOCIETY
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Erscheinungsdatum:01.01.2000
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Format / Umfang:12 pages
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ISSN:
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Medientyp:Aufsatz (Zeitschrift)
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Format:Print
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Sprache:Englisch
- Neue Suche nach: 615
- Weitere Informationen zu Dewey Decimal Classification
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Klassifikation:
DDC: 615 -
Datenquelle:
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Inhaltsverzeichnis – Band 43
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- 342
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A Novel, Potent, and Selective 5-HT7 Antagonist: (R)-3-(2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl)phenol (SB-269970)Lovell, Peter J. / Bromidge, Steven M. / Dabbs, Steven / Duckworth, D. Malcolm / Forbes, Ian T. / Jennings, Andrew J. / King, Frank D. / Middlemiss, Derek N. / Rahman, Shirley K. / Saunders, Damian V. et al. | 2000
- 346
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α-Substituted N-(Sulfonamido)alkyl-β-aminotetralins: Potent and Selective Neuropeptide Y Y5 Receptor AntagonistsYoungman, Mark A. / McNally, James J. / Lovenberg, Timothy W. / Reitz, Allen B. / Willard, Nicole M. / Nepomuceno, Diane H. / Wilson, Sandy J. / Crooke, Jeffrey J. / Rosenthal, Daniel / Vaidya, Anil H. et al. | 2000
- 346
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Communications - a-Substituted N-(Sulfonamido)alkyl-b-aminotetralins: Potent and Selective Neuropeptide Y Y5 Receptor AntagonistsYoungman, Mark A. et al. | 2000
- 346
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alpha-Substituted N-(Sulfonamido)alkyl-beta-aminotetralins: Potent and Selective Neuropeptide Y Y5 Receptor AntagonistsYoungman, M. A. / McNally, J. J. / Lovenberg, T. W. / Reitz, A. B. / Willard, N. M. / Nepomuceno, D. H. / Wilson, S. J. / Crooke, J. J. / Rosennthal, D. / Vaidya, A. H. et al. | 2000
- 351
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Expedited Articles - Discovery of a Novel Dopamine Transporter Inhibitor, 4-Hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-Methylphenyl Ketone, as a Potential Cocaine Antagonist through 3D-Database Pharmacophore Searching. Molecular Modeling, Structure -- Activity Relationships, and Behavioral Pharmacological StudiesWang, Shaomeng et al. | 2000
- 351
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Discovery of Novel Dopamine Transporter Inhibitor, 4-Hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-Methylyphenyl ketone, as a Pontential Cocaine Antagonist through 3D-Database Pharmacophore Searching. Molecular Modeling, Structure-Activity Relationships, and Behavioral Pharmacological StudiesWang, S. / Sakamuri, S. / Enyedy, I. J. / Kozikowski, A. P. / Deschaux, O. / Bangyopadhyay, B. C. / Tella, S. R. / Zaman, W. A. / Johnson, K. M. et al. | 2000
- 351
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Discovery of a Novel Dopamine Transporter Inhibitor, 4-Hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-Methylphenyl Ketone, as a Potential Cocaine Antagonist through 3D-Database Pharmacophore Searching. Molecular Modeling, Structure−Activity Relationships, and Behavioral Pharmacological StudiesWang, Shaomeng / Sakamuri, Sukumar / Enyedy, Istvan J. / Kozikowski, Alan P. / Deschaux, Olivier / Bandyopadhyay, Bidhan C. / Tella, Srihari R. / Zaman, Wahiduz A. / Johnson, Kenneth M. et al. | 2000
- 361
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Structural Basis of the Thrombin Selectivity of a Ligand That Contains the Constrained Arginine Minic (2S)-2-Amino-(3S)-3-(1-carbamimidoylpiperidin-3-yl)-propanoic Acid at P1Narashihan, L. S. / Rubin, J. R. / Holland, D. R. / Plummer, J. S. / Rapundalo, S. T. / Edmunds, J. E. / St-Denis, Y. / Siddique, M. A. / Humblet, C. et al. | 2000
- 361
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Articles - Structural Basis of the Thrombin Selectivity of a Ligand That Contains the Constrained Arginine Mimic (2S)-2-Amino-(3S)-3-(1-carbamimidoyl-piperidin-3-yl)-propanoic Acid at P1Narasimhan, Lakshmi S. et al. | 2000
- 361
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Structural Basis of the Thrombin Selectivity of a Ligand That Contains the Constrained Arginine Mimic (2S)-2-Amino-(3S)-3-(1-carbamimidoyl- piperidin-3-yl)-propanoic Acid at P1Narasimhan, Lakshmi S. / Rubin, J. Ronald / Holland, Debra R. / Plummer, Janet S. / Rapundalo, Stephen T. / Edmunds, Jeremy E. / St-Denis, Yves / Siddiqui, M. Arshad / Humblet, Christine et al. | 2000
- 369
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Articles - Design and Synthesis of Piperazine-Based Matrix Metalloproteinase InhibitorsCheng, Menyan et al. | 2000
- 369
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Design and Synthesis of Piperazine-Based Matrix Metalloproteinase InhibitorsCheng, Menyan / De, Biswanath / Pikul, Stanislaw / Almstead, Neil G. / Natchus, Michael G. / Anastasio, Melanie V. / McPhail, Sara J. / Snider, Catherine E. / Taiwo, Yetunde O. / Chen, Longyin et al. | 2000
- 381
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Articles - Molecular Docking Reveals a Novel Binding Site Model for Fentanyl at the m-Opioid ReceptorSubramanian, Govindan et al. | 2000
- 381
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Molecular Docking Reveals a Novel Binding Site Model for Fentanyl at the mu-Opioid ReceptorSubramanian, G. / Paterlini, M. G. / Portoghese, P. S. / Ferguson, D. M. et al. | 2000
- 381
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Molecular Docking Reveals a Novel Binding Site Model for Fentanyl at the μ-Opioid ReceptorSubramanian, Govindan / Paterlini, M. Germana / Portoghese, Philip S. / Ferguson, David M. et al. | 2000
- 392
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Derivation of Pharmacophore and CoMFA Models for Leukotriene D~4 Receptor Antagonists of the Quinoliny(bridged)aryl SeriesPalomer, A. / Pascual, J. / Cabre, F. / Garcia, M. L. / Mauleon, D. et al. | 2000
- 392
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Articles - Derivation of Pharmacophore and CoMFA Models for Leukotriene D4 Receptor Antagonists of the Quinolinyl(bridged)aryl SeriesPalomer, Albert et al. | 2000
- 392
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Derivation of Pharmacophore and CoMFA Models for Leukotriene D4 Receptor Antagonists of the Quinolinyl(bridged)aryl SeriesPalomer, Albert / Pascual, Jaume / Cabré,, Francesc / García, M. Lluïsa / Mauleón, David et al. | 2000
- 401
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Successful Virtual Screening of a Chemical Database for Farnesyltransferase Inhibitor LeadsPerola, Emanuele / Xu, Kun / Kollmeyer, Thomas M. / Kaufmann, Scott H. / Prendergast, Franklyn G. / Pang, Yuan-Ping et al. | 2000
- 401
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Articles - Successful Virtual Screening of a Chemical Database for Farnesyltransferase Inhibitor LeadsPerola, Emanuele et al. | 2000
- 409
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Articles - Syntheses and Structure -- Activity Relationships of 5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline Derivatives with Retinoic Acid Receptor a Agonistic ActivityKikuchi, Kouichi et al. | 2000
- 409
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Syntheses and Structure−Activity Relationships of 5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline Derivatives with Retinoic Acid Receptor α Agonistic ActivityKikuchi, Kouichi / Hibi, Shigeki / Yoshimura, Hiroyuki / Tokuhara, Naoki / Tai, Kenji / Hida, Takayuki / Yamauchi, Toshihiko / Nagai, Mitsuo et al. | 2000
- 409
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Syntheses and Structure-Activity Relationships of 5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline Derivatives with Retinoic Acid Receptor alpha Agonistic ActivityKikuchi, K. / Hibi, S. / Yoshimura, H. / Tokuhara, N. / Tai, K. / Hida, T. / Yamauchi, T. / Nagai, M. et al. | 2000
- 420
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Synthesis, Molecular Modeling, and Pharmacological Testing of Bis-Quinolinium Cyclophanes: Potent, Non-Peptidic Blockers of the Apamin-Sensitive Ca2+-Activated K+ ChannelCampos Rosa, Joaquin / Galanakis, Dimitrios / Piergentili, Alessandro / Bhandari, Kalpana / Ganellin, C. Robin / Dunn, Philip M. / Jenkinson, Donald H. et al. | 2000
- 420
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Articles - Synthesis, Molecular Modeling, and Pharmacological Testing of Bis-Quinolinium Cyclophanes: Potent, Non-Peptidic Blockers of the Apamin-Sensitive Ca2+-Activated K+ ChannelRosa, Joaquin Campos et al. | 2000
- 432
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Articles - Synthesis and in Vitro and in Vivo Functional Studies of Ortho-Substituted Phenylpiperazine and N-Substituted 4-N-(o-Methoxyphenyl)aminopiperidine Analogues of WAY100635Mensonides-Harsema, Marguérite M. et al. | 2000
- 432
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Synthesis and in Vitro and in Vivo Functional Studies of Ortho-Substituted Phenylpiperazine and N-Substituted 4-N-(o-Methoxyphenyl)aminopiperidine Analogues of WAY100635Mensonides-Harsema, Marguérite M. / Liao, Yi / Böttcher, Henning / Bartoszyk, Gerd D. / Greiner, Hartmunt E. / Harting, Jürgen / de Boer, Peter / Wikström, Håkan V. et al. | 2000
- 440
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Water-Soluble Phosphate Prodrugs of 1-Propargyl-8-styrylxanthine Derivatives, A2A-Selective Adenosine Receptor Antagonists †Sauer, Roland / Maurinsh, Juris / Reith, Ulrike / Fülle, Friederike / Klotz, Karl-Norbert / Müller, Christa E. et al. | 2000
- 440
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Articles - Water-Soluble Phosphate Prodrugs of 1-Propargyl-8-styrylxanthine Derivatives, A2A-Selective Adenosine Receptor AntagonistsSauer, Roland et al. | 2000
- 449
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4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2,4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: A Potent, Orally Bioavailable CRF1 Receptor AntagonistHe, Liqi / Gilligan, Paul J. / Zaczek, Robert / Fitzgerald, Lawrence W. / McElroy, John / Shen, H-S. L. / Saye, Jo Anne / Kalin, Ned H. / Shelton, Steven / Christ, David et al. | 2000
- 449
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Articles - 4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2,4-dichlorophenyl)- pyrazolo(1,5-a)-1,3,5-triazine: A Potent, Orally Bioavailable CRF1 Receptor AntagonistHe, Liqi et al. | 2000
- 449
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4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2,4-dichlorophenyl) pyrazolo[1,5-alpha]-1,3,5-triazine: A Potent, Orally Bioavailable CRF~1 Receptor AntagonistHe, L. / Gilligan, P. J. / Zaczek, R. / Fitzgerald, L. W. / McElroy, J. / Shen, H. L. / Saye, J. A. / Kalin, N. H. / Shelton, S. / Christ, D. et al. | 2000
- 457
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Design of Cancer-Specific Antitumor Agents Based on Aziridinylcyclopent[b]indoloquinonesXing, Chengguo / Wu, Ping / Skibo, Edward B. / Dorr, Robert T. et al. | 2000
- 457
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Articles - Design of Cancer-Specific Antitumor Agents Based on Aziridinylcyclopent(b)indoloquinonesXing, Chengguo et al. | 2000
- 467
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Acid-Catalyzed Degradation of Clarithromycin and Erythromycin B: A Comparative Study Using NMR SpectroscopyMordi, Mohd N. / Pelta, Michelle D. / Boote, Valerie / Morris, Gareth A. / Barber, Jill et al. | 2000
- 467
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Articles - Acid-Catalyzed Degradation of Clarithromycin and Erythromycin B: A Comparative Study Using NMR SpectroscopyMordi, Mohd N. et al. | 2000
- 475
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Drug Delivery Systems Based on Trimethyl Lock Lactonization: Poly(ethylene glycol) Prodrugs of Amino-Containing CompoundsGreenwald, Richard B. / Choe, Yun H. / Conover, Charles D. / Shum, Kwok / Wu, Dechun / Royzen, Maksim et al. | 2000
- 475
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Articles - Drug Delivery Systems Based on Trimethyl Lock Lactonization: Poly(ethylene glycol) Prodrugs of Amino-Containing CompoundsGreenwald, Richard B. et al. | 2000
- 488
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Potent and Selective Non-Peptidic Inhibitors of Endothelin-Converting Enzyme-1 with Sustained Duration of ActionDe Lombaert, Stéphane / Blanchard, Louis / Stamford, Lisa B. / Tan, Jenny / Wallace, Eli M. / Satoh, Yoshitaka / Fitt, John / Hoyer, Denton / Simonsbergen, David / Moliterni, John et al. | 2000
- 488
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Articles - Potent and Selective Non-Peptidic Inhibitors of Endothelin-Converting Enzyme-1 with Sustained Duration of ActionLombaert, Stéphane De et al. | 2000
- 505
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Articles - Antimalarial Activity of Compounds Interfering with Plasmodium falciparum Phospholipid Metabolism: Comparison between Mono- and Bisquaternary Ammonium SaltsCalas, Michèle et al. | 2000
- 505
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Antimalarial Activity of Compounds Interfering with Plasmodium falciparum Phospholipid Metabolism: Comparison between Mono- and Bisquaternary Ammonium Salts ‡Calas, Michèle / Ancelin, Marie L. / Cordina, Gérard / Portefaix, Philippe / Piquet, Gilles / Vidal-Sailhan, Valérie / Vial, Henri et al. | 2000
- 517
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New Selective and Potent 5-HT1B/1D Antagonists: Chemistry and Pharmacological Evaluation of N-Piperazinylphenyl Biphenylcarboxamides and BiphenylsulfonamidesLiao, Yi / Böttcher, Henning / Harting, Jürgen / Greiner, Hartmut / van Amsterdam, Christoph / Cremers, Thomas / Sundell, Staffan / März, Joachim / Rautenberg, Wilfried / Wikström, Håkan et al. | 2000
- 517
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Brief Articles - New Selective and Potent 5-HT1B-1D Antagonists: Chemistry and Pharmacological Evaluation of N-Piperazinylphenyl Biphenylcarboxamides and BiphenylsulfonamidesLiao, Yi et al. | 2000
- 526
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Book Reviews Process Chemistry in the Pharmaceutical IndustryNovack, Vance et al. | 2000
- 526
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Process Chemistry in the Pharmaceutical IndustryNovack, V. et al. | 2000
- 526
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Process Chemistry in the Pharmaceutical Industry Edited by Kumar Gadamasetti. Marcel Dekker, Inc., New York. 1999. xii + 474 pp. 18 × 26 cm. ISBN 0-8247-1981-6. $195.00.Novack, Vance et al. | 2000
- 527
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The PPARs: From Orphan Receptors to Drug Discovery †Willson, Timothy M. / Brown, Peter J. / Sternbach, Daniel D. / Henke, Brad R. et al. | 2000
- 527
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Perspectives - The PPARs: From Orphan Receptors to Drug DiscoveryWillson, Timothy M. et al. | 2000
- 551
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Novel Ligands Lacking a Positive Charge for the δ- and μ-Opioid ReceptorsSchiller, Peter W. / Berezowska, Irena / Nguyen, Thi M.-D. / Schmidt, Ralf / Lemieux, Carole / Chung, Nga N. / Falcone-Hindley, Margaret L. / Yao, Wenqing / Liu, Josephine / Iwama, Seiji et al. | 2000
- 551
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Novel Ligands Lacking a Positive Charge for the delta-and mu-Opioid ReceptorsSchiller, P. W. / Berezowska, I. / Nguyen, T. M. / Schmidt, R. / Lemieux, C. / Chung, N. N. / Falcone-Hindley, M. L. / Yao, W. / Liu, J. / Iwama, S. et al. | 2000
- 551
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Expedited Articles - Novel Ligands Lacking a Positive Charge for the d- and m-Opioid ReceptorsSchiller, Peter W. et al. | 2000
- 560
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Articles - Phenyl b-Methoxyacrylates: A New Antimalarial PharmacophoreAlzeer, Jawad et al. | 2000
- 560
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Phenyl beta-Methoxyacrylates: A New Antimalarial PharmacophoreAlzeer, J. / Chollet, J. / Heinze-Krauss, I. / Hubschwerlen, C. / Matile, H. / Ridley, R. G. et al. | 2000
- 560
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Phenyl β-Methoxyacrylates: A New Antimalarial PharmacophoreAlzeer, Jawad / Chollet, Jacques / Heinze-Krauss, Ingrid / Hubschwerlen, Christian / Matile, Hugues / Ridley, Robert G. et al. | 2000
- 569
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Articles - Opiate Aromatic Pharmacophore Structure-Activity Relationships in CTAP Analogues Determined by Topographical Bias, Two-Dimensional NMR, and Biological Activity AssaysBonner, G.Gregg et al. | 2000
- 569
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Opiate Aromatic Pharmacophore Structure−Activity Relationships in CTAP Analogues Determined by Topographical Bias, Two-Dimensional NMR, and Biological Activity AssaysBonner, G. Gregg / Davis, Peg / Stropova, Dagmar / Edsall, Sidney / Yamamura, Henry I. / Porreca, Frank / Hruby, Victor J. et al. | 2000
- 581
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Chiral Nonsteroidal Affinity Ligands for the Androgen Receptor. 1. Bicalutamide Analogues Bearing Electrophilic Groups in the B Aromatic RingKirkovsky, Leonid / Mukherjee, Arnab / Yin, Donghua / Dalton, James T. / Miller, Duane D. et al. | 2000
- 581
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Articles - Chiral Nonsteroidal Affinity Ligands for the Androgen Receptor. 1. Bicalutamide Analogues Bearing Electrophilic Groups in the B Aromatic RingKirkovsky, Leonid et al. | 2000
- 591
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Synthesis and Human beta-Adrenoceptor Activity of 1-(3,5-Diiodo-4-methoxybenzyl)-1,2,3,4-tetra-hydroisoquinolin-6-ol Derivatives in VitroHe, Y. / Nikulin, V. I. / Vansal, S. S. / Feller, D. R. / Miller, D. D. et al. | 2000
- 591
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Synthesis and Human β-Adrenoceptor Activity of 1-(3,5-Diiodo-4- methoxybenzyl)-1,2,3,4-tetrahydroisoquinolin-6-ol Derivatives in VitroHe, Yali / Nikulin, Victor I. / Vansal, Sandeep S. / Feller, Dennis R. / Miller, Duane D. et al. | 2000
- 591
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Articles - Synthesis and Human b-Adrenoceptor Activity of 1-(3,5-Diiodo-4-methoxybenzyl)-1,2,3,4-tetra-hydroisoquinolin-6-ol Derivatives in VitroHe, Yali et al. | 2000
- 599
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Articles - Binding and Preliminary Evaluation of 5-Hydroxy- and 10-Hydroxy-2,3,12,12a-tetra-hydro-1H-(1lbenzoxepino(2,3,4- ij)isoquinolines as Dopamine Receptor LigandsClaudi, Francesco et al. | 2000
- 599
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Binding and Preliminary Evaluation of 5-Hydroxy- and 10-Hydroxy-2,3,12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-i j]isoquinolines as Dopamine Receptor LigandsClaudi, Francesco / Di Stefano, Antonio / Napolitani, Fabrizio / Cingolani, Gian Mario / Giorgioni, Gianfabio / Fontenla, Josè A. / Montenegro, Gisela Y. / Rivas, Maria E. / Rosa, Elizabeth / Michelotto, Barbara et al. | 2000
- 609
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Hypocholesterolemic and Hypolipidemic Activity of Some Novel Morpholine Derivatives with Antioxidant ActivityChrysselis, Michael C. / Rekka, Eleni A. / Kourounakis, Panos N. et al. | 2000
- 609
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Articles - Hypocholesterolemic and Hypolipidemic Activity of Some Novel Morpholine Derivatives with Antioxidant ActivityChrysselis, Michael C. et al. | 2000
- 613
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Steroidal Affinity Labels of the Estrogen Receptor alpha. 4. Electrophilic 11beta-Aryl Derivatives of EstradiolAliau, S. / Delettre, G. / Mattras, H. / El Garrouj, D. / Nique, F. / Teutsch, G. / Jean-Louis, B. et al. | 2000
- 613
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Articles - Steroidal Affinity Labels of the Estrogen Receptor a. 4. Electrophilic 11b-Aryl Derivatives of EstradiolAliau, Sigrid et al. | 2000
- 613
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Steroidal Affinity Labels of the Estrogen Receptor α. 4. Electrophilic 11β-Aryl Derivatives of EstradiolAliau, Sigrid / Delettre, Georges / Mattras, Hélène / El Garrouj, Driss / Nique, François / Teutsch, Georges / Borgna, Jean-Louis et al. | 2000
- 629
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Inhibitors of Topoisomerase II Based on the Benzodiimidazole and Dipyrroloimidazobenzimidazole Ring Systems: Controlling DT-Diaphorase Reductive Inactivation with Steric BulkSchulz, William G. / Skibo, Edward B. et al. | 2000
- 629
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Articles - Inhibitors of Topoisomerase II Based on the Benzodiimidazole and Dipyrroloimidazobenzimidazole Ring Systems: Controlling DT-Diaphorase Reductive Inactivation with Steric BulkSchulz, William G. et al. | 2000
- 639
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Synthesis, Biodistribution, and Primate Imaging of Fluorine-18 Labeled 2beta-Carbo-1'-fluoro-2-propoxy-3beta-(4-chlorophenyl)tropanes. Ligands for the Imaging of Dopamine Transporters by Positron Emission TomographyXing, D. / Chen, P. / Keil, R. / Kilts, C. D. / Shi, B. / Camp, V. M. / Malveaux, G. / Ely, T. / Owens, M. J. / Votaw, J. et al. | 2000
- 639
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Synthesis, Biodistribution, and Primate Imaging of Fluorine-18 Labeled 2β-Carbo-1‘-fluoro-2-propoxy-3β-(4-chlorophenyl)tropanes. Ligands for the Imaging of Dopamine Transporters by Positron Emission TomographyXing, Dongxia / Chen, Ping / Keil, Robert / Kilts, Clinton D. / Shi, Bing / Camp, Vernon M. / Malveaux, Gene / Ely, Timothy / Owens, Michael J. / Votaw, John et al. | 2000
- 639
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Articles - Synthesis, Biodistribution, and Primate Imaging of Fluorine-18 Labeled 2b-Carbo-1'-fluoro-2-propoxy-3b- (4-chlorophenyl)tropanes. Ligands for the Imaging of Dopamine Transporters by Positron Emission TomographyXing, Dongxia et al. | 2000
- 649
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Diamino Benzo[b]thiophene Derivatives as a Novel Class of Active Site Directed Thrombin Inhibitors. 5. Potency, Efficacy, and Pharmacokinetic Properties of Modified C-3 Side Chain DerivativesSall, Daniel J. / Bailey, Dianna L. / Bastian, Jolie A. / Buben, John A. / Chirgadze, Nickolay Y. / Clemens-Smith, Amy C. / Denney, Michael L. / Fisher, Matthew J. / Giera, Deborah D. / Gifford-Moore, Donetta S. et al. | 2000
- 649
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Articles - Diamino Benzo(b)thiophene Derivatives as a Novel Class of Active Site Directed Thrombin Inhibitors. 5. Potency, Efficacy, and Pharmacokinetic Properties of Modified C-3 Side Chain DerivativesSall, Daniel J. et al. | 2000
- 664
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Inhibitors of Tripeptidyl Peptidase II. 2. Generation of the First Novel Lead Inhibitor of Cholecystokinin-8-Inactivating Peptidase: A Strategy for the Design of Peptidase Inhibitors ‡Ganellin, C. Robin / Bishop, Paul B. / Bambal, Ramesh B. / Chan, Suzanne M. T. / Law, James K. / Marabout, Benoit / Luthra, Pratibha Mehta / Moore, Andrew N. J. / Peschard, Olivier / Bourgeat, Pierre et al. | 2000
- 664
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Articles - Inhibitors of Tripeptidyl Peptidase II. 2. Generation of the First Novel Lead Inhibitor of Cholecystokinin-8-Inactivating Peptidase: A Strategy for the Design of Peptidase InhibitorsGanellin, C.Robin et al. | 2000
- 675
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Palladium-Catalyzed Cross-Coupling Reactions for the Synthesis of 6,8-Disubstituted 1,7-Naphthyridines: A Novel Class of Potent and Selective Phosphodiesterase Type 4D InhibitorsHersperger, Rene / Bray-French, Katharine / Mazzoni, Lazzaro / Müller, Thomas et al. | 2000
- 675
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Articles - Palladium-Catalyzed Cross-Coupling Reactions for the Synthesis of 6,8-Disubstituted 1,7-Naphthyridines: A Novel Class of Potent and Selective Phosphodiesterase Type 4D InhibitorsHersperger, Rene et al. | 2000
- 683
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Articles - Benzyl Derivatives of 2,1,3-Benzo- and Benzothieno(3,2-a)thiadiazine 2,2-Dioxides: First Phosphodiesterase 7 InhibitorsMartinez, Ana et al. | 2000
- 683
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Benzyl Derivatives of 2,1,3-Benzo- and Benzothieno[3,2-alpha]thiadiazine 2,2-Dioxides: First Phosphodiesterase 7 InhibitorsMartinez, A. / Castro, A. / Gil, C. / Miralpeix, M. / Segarra, V. / Domenech, T. / Beleta, J. / Palacios, J. M. / Ryder, H. / Miro, X. et al. | 2000
- 683
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Benzyl Derivatives of 2,1,3-Benzo- and Benzothieno[3,2-a]thiadiazine 2,2-Dioxides: First Phosphodiesterase 7 InhibitorsMartínez, Ana / Castro, Ana / Gil, Carmen / Miralpeix, Montserrat / Segarra, Victor / Doménech, Teresa / Beleta, Jorge / Palacios, Jose M. / Ryder, Hamish / Miró, Xavier et al. | 2000
- 690
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Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic Acids as Leukotriene Biosynthesis InhibitorsKolasa, Teodozyj / Gunn, David E. / Bhatia, Pramila / Woods, Keith W. / Gane, Todd / Stewart, Andrew O. / Bouska, Jennifer B. / Harris, Richard R. / Hulkower, Keren I. / Malo, Peter E. et al. | 2000
- 690
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Articles - Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic Acids as Leukotriene Biosynthesis InhibitorsKolasa, Teodozyj et al. | 2000
- 706
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Articles - A New Class of Conformationally Rigid Analogues of 4-Amino-5-halopentanoic Acids, Potent Inactivators of g-Aminobutyric Acid AminotransferaseQiu, Jian et al. | 2000
- 706
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A New Class of Conformationally Rigid Analogues of 4-Amino-5-halopentanoic Acids, Potent Inactivators of γ-Aminobutyric Acid AminotransferaseQiu, Jian / Silverman, Richard B. et al. | 2000
- 706
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A New Class of Conformationally Rigid Analogues of 4-Amino-5-halopentanoic Acids, Potent Inactivators of gamma-Aminobutyric Acid AminotransferaseQiu, J. / Silverman, R. B. et al. | 2000
- 721
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Structure−Activity Relationship Studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a Potent Inhibitor of Leukotriene A4 (LTA4) HydrolasePenning, Thomas D. / Chandrakumar, Nizal S. / Chen, Barbara B. / Chen, Helen Y. / Desai, Bipin N. / Djuric, Stevan W. / Docter, Stephen H. / Gasiecki, Alan F. / Haack, Richard A. / Miyashiro, Julie M. et al. | 2000
- 721
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Articles - Structure-Activity Relationship Studies on 1-(2-(4-Phenylphenoxy)ethyl)pyrrolidine (SC-22716), a Potent Inhibitor of Leukotriene A4 (LTA4) HydrolasePenning, Thomas D. et al. | 2000
- 736
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Articles - The Cyclohexene Ring System as a Furanose Mimic: Synthesis and Antiviral Activity of Both Enantiomers of CyclohexenylguanineWang, Jing et al. | 2000
- 736
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The Cyclohexene Ring System as a Furanose Mimic: Synthesis and Antiviral Activity of Both Enantiomers of CyclohexenylguanineWang, Jing / Froeyen, Matheus / Hendrix, Chris / Andrei, Graciela / Snoeck, Robert / De Clercq, Erik / Herdewijn, Piet et al. | 2000
- 746
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Acyclic Analogues of Deoxyadenosine 3‘,5‘-Bisphosphates as P2Y1 Receptor AntagonistsKim, Yong-Chul / Gallo-Rodriguez, Carola / Jang, Soo-Yeon / Nandanan, Erathodiyil / Adams, Mary / Harden, T. Kendall / Boyer, José L. / Jacobson, Kenneth A. et al. | 2000
- 746
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Articles - Acyclic Analogues of Deoxyadenosine 3',5'-Bisphosphates as P2Y1 Receptor AntagonistsKim, Yong-Chul et al. | 2000
- 756
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Conjugated Enynes as Nonaromatic Catechol Bioisosteres: Synthesis, Binding Experiments, and Computational Studies of Novel Dopamine Receptor Agonists Recognizing Preferentially the D3 SubtypeHübner, Harald / Haubmann, Christian / Utz, Wolfgang / Gmeiner, Peter et al. | 2000
- 756
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Brief Articles - Conjugated Enynes as Nonaromatic Catechol Bioisosteres: Synthesis, Binding Experiments, and Computational Studies of Novel Dopamine Receptor Agonists Recognizing Preferentially the D3 SubtypeHübner, Harald et al. | 2000
- 763
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Drugs and the Pharmaceutical Sciences. Volume 100. New Drug Approval Process, 3rd Edition Edited by Richard A. Guarino. Marcel Dekker, Inc., New York. 1999. xxxiii + 471 pp. 16 × 23.5 cm. ISBN 0-8247-0308-1. $185.00.Ronsen, Bruce et al. | 2000
- 763
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Book Reviews - Drugs and the Pharmaceutical Sciences. Volume 100. New Drug Approval Process, 3rd EditionRonsen, Bruce et al. | 2000
- 764
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Additions and Corrections - Three-Dimensional Quantitative Structure-Activity Relationship Study on Cyclic Urea Derivatives as HIV-1 Protense Inhibitors: Application of Comparative Molecular Field AnalysisDebnath, Asim Kumar et al. | 2000
- 765
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Communications - a2 Adrenoceptor Agonists as Potential Analgesic Agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene as a High-Affinity Ligand for the a2D Adrenergic ReceptorRoss, Tina M. et al. | 2000
- 765
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alpha~2 Adrenoceptor Agonists as Potential Analgesic Agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene as a High-Affinity Ligand for the alpha~2~D Adrenergic ReceptorRoss, T. M. / Jetter, M. C. / McDonnell, M. E. / Boyd, R. E. / Connelly, C. D. / Martinez, R. P. / Lewis, M. A. / Codd, E. E. / Raffa, R. B. / Reitz, A. B. et al. | 2000
- 765
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α2 Adrenoceptor Agonists as Potential Analgesic Agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene as a High-Affinity Ligand for the α2D Adrenergic ReceptorRoss, Tina M. / Jetter, Michele C. / McDonnell, Mark E. / Boyd, Robert E. / Connelly, Charlene D. / Martinez, Rebecca P. / Lewis, Martin A. / Codd, Ellen E. / Raffa, Robert B. / Reitz, Allen B. et al. | 2000
- 769
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Communications - 1-(2-Nitrophenyl)thiosemicarbazides: A Novel Class of Potent, Orally Active Non-Peptide Antagonist for the Bradykinin B2 ReceptorDziadulewicz, Edward K. et al. | 2000
- 769
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1-(2-Nitrophenyl)thiosemicarbazides: A Novel Class of Potent, Orally Active Non-Peptide Antagonist for the Bradykinin B2 ReceptorDziadulewicz, Edward K. / Ritchie, Timothy J. / Hallett, Allan / Snell, Christopher R. / Ko, Soo Y. / Wrigglesworth, Roger / Hughes, Glyn A. / Dunstan, Andrew R. / Bloomfield, Graham C. / Drake, Gillian S. et al. | 2000
- 769
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1-(2-Nitrophenyl)thiosemicarbazides: A Novel Class of Potent, Orally Active Non-Peptide Antogonist for the Bradykinin B~2 ReceptorDziadulewicz, E. K. / Ritchie, T. J. / Hallett, A. / Snell, C. R. / Ko, S. Y. / Wrigglesworth, R. / Hughes, G. A. / Dunstan, A. R. / Bloomfield, G. C. / Drake, G. S. et al. | 2000
- 772
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Dual Function Glutamate-Related Ligands: Discovery of a Novel, Potent Inhibitor of Glutamate Carboxypeptidase II Possessing mGluR3 Agonist ActivityNan, Fajun / Bzdega, Tomasz / Pshenichkin, Sergey / Wroblewski, Jarda T. / Wroblewska, Barbara / Neale, Joseph H. / Kozikowski, Alan P. et al. | 2000
- 772
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Communications - Dual Function Glutamate-Related Ligands: Discovery of a Novel, Potent Inhibitor of Glutamate Carboxypeptidase II Possessing mGluR3 Agonist ActivityNan, Fajun et al. | 2000
- 775
-
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, Valdecoxib: A Potent and Selective Inhibitor of COX-2Talley, John J. / Brown, David L. / Carter, Jeffery S. / Graneto, Matthew J. / Koboldt, Carol M. / Masferrer, Jaime L. / Perkins, William E. / Rogers, Roland S. / Shaffer, Alexander F. / Zhang, Yan Y. et al. | 2000
- 775
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Communications - 4-(5-Methyl-3-phenylisoxazol-4-yl)-benzenesulfonamide, Valdecoxib: A Potent and Selective Inhibitor of COX-2Talley, John J. et al. | 2000
- 778
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Articles - Potent Anti-HIV (Type 1 and Type 2) Activity of Polyoxometalates: Structure-Activity Relationship and Mechanism of ActionWitvrouw, Myriam et al. | 2000
- 778
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Potent Anti-HIV (Type 1 and Type 2) Activity of Polyoxometalates: Structure−Activity Relationship and Mechanism of ActionWitvrouw, Myriam / Weigold, Helmut / Pannecouque, Christophe / Schols, Dominique / De Clercq, Erik / Holan, George et al. | 2000
- 784
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Articles - Design of Potent Dicyclic (4-10-5-8) Gonadotropin Releasing Hormone (GnRH) AntagonistsRivier, Jean E. et al. | 2000
- 784
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Design of Potent Dicyclic (4−10/5−8) Gonadotropin Releasing Hormone (GnRH) AntagonistsRivier, Jean E. / Struthers, R. Scott / Porter, John / Lahrichi, Sabine L. / Jiang, Guangcheng / Cervini, Laura A. / Ibea, Michel / Kirby, Dean A. / Koerber, Steven C. / Rivier, Catherine L. et al. | 2000
- 797
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Design of Monocyclic (1−3) and Dicyclic (1−3/4−10) Gonadotropin Releasing Hormone (GnRH) Antagonists †Rivier, Jean E. / Porter, John / Cervini, Laura A. / Lahrichi, Sabine L. / Kirby, Dean A. / Struthers, R. Scott / Koerber, Steven C. / Rivier, Catherine L. et al. | 2000
- 797
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Articles - Design of Monocyclic (1-3) and Dicyclic (1-3-4-10) Gonadotropin Releasing Hormone (GnRH) AntagonistsRivier, Jean E. et al. | 2000
- 807
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Design of Potent Dicyclic (1−5/4−10) Gonadotropin Releasing Hormone (GnRH) Antagonists †Rivier, Jean E. / Jiang, Guangcheng / Struthers, R. Scott / Koerber, Steven C. / Porter, John / Cervini, Laura A. / Kirby, Dean A. / Craig, A. Grey / Rivier, Catherine L. et al. | 2000
- 807
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Articles - Design of Potent Dicyclic (1-5-4-10) Gonadotropin Releasing Hormone (GnRH) AntagonistsRivier, Jean E. et al. | 2000
- 819
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Consensus Bioactive Conformation of Cyclic GnRH Antagonists Defined by NMR and Molecular Modeling †Koerber, Steven C. / Rizo, Josep / Struthers, R. Scott / Rivier, Jean E. et al. | 2000
- 819
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Articles - Consensus Bioactive Conformation of Cyclic GnRH Antagonists Defined by NMR and Molecular ModelingKoerber, Steven C. et al. | 2000
- 829
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Articles - Synthesis, Biological Activity, and Molecular Modeling of Ribose-Modified Deoxyadenosine Bisphosphate Analogues as P2Y1 Receptor LigandsNandanan, Erathodiyil et al. | 2000
- 829
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Synthesis, Biological Activity, and Molecular Modeling of Ribose-Modified Deoxyadenosine Bisphosphate Analogues as P2Y1 Receptor LigandsNandanan, Erathodiyil / Jang, Soo-Yeon / Moro, Stefano / Kim, Hea Ok / Siddiqui, Maqbool A. / Russ, Pamela / Marquez, Victor E. / Busson, Roger / Herdewijn, Piet / Harden, T. Kendall et al. | 2000
- 843
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Articles - 5,6-Dihydropyran-2-ones Possessing Various Sulfonyl Functionalities: Potent Nonpeptidic Inhibitors of HIV ProteaseBoyer, Frederick E. et al. | 2000
- 843
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5,6-Dihydropyran-2-ones Possessing Various Sulfonyl Functionalities: Potent Nonpeptidic Inhibitors of HIV ProteaseBoyer, Frederick E. / Vara Prasad, J. V. N. / Domagala, John M. / Ellsworth, Edmund L. / Gajda, Christopher / Hagen, Susan E. / Markoski, Larry J. / Tait, Bradley D. / Lunney, Elizabeth A. / Palovsky, Alexander et al. | 2000
- 859
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1,2-Dibenzamidobenzene Inhibitors of Human Factor XaHerron, David K. / Goodson, Theodore / Wiley, Michael R. / Weir, Leonard C. / Kyle, Jeffrey A. / Yee, Ying K. / Tebbe, Ann Louise / Tinsley, Jennifer M. / Mendel, David / Masters, John J. et al. | 2000
- 859
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Articles - 1,2-Dibenzamidobenzene Inhibitors of Human Factor XaHerron, David K. et al. | 2000
- 873
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Articles - N2-Aroylanthranilamide Inhibitors of Human Factor XaYee, Ying K. et al. | 2000
- 873
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N 2-Aroylanthranilamide Inhibitors of Human Factor XaYee, Ying K. / Tebbe, Anne Louise / Linebarger, Jared H. / Beight, Douglas W. / Craft, Trelia J. / Gifford-Moore, Donetta / Goodson, Theodore / Herron, David K. / Klimkowski, Valentine J. / Kyle, Jeffrey A. et al. | 2000
- 883
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Structure-Based Design of Potent, Amidine-Derived Inhibitors of Factor Xa: Evaluation of Selectivity, Anticoagulant Activity, and Antithrombotic ActivityWiley, Michael R. / Weir, Leonard C. / Briggs, Steven / Bryan, Nancy A. / Buben, John / Campbell, Charles / Chirgadze, Nickolay Y. / Conrad, Richard C. / Craft, Trelia J. / Ficorilli, James V. et al. | 2000
- 883
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Articles - Structure-Based Design of Potent, Amidine-Derived Inhibitors of Factor Xa: Evaluation of Selectivity, Anticoagulant Activity, and Antithrombotic ActivityWiley, Michael R. et al. | 2000
- 900
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Articles - Selective ETA Antagonists. 5. Discovery and Structure-Activity Relationships of Phenoxyphenylacetic Acid DerivativesAstles, Peter C. et al. | 2000
- 900
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Selective ETA Antagonists. 5. Discovery and Structure−Activity Relationships of Phenoxyphenylacetic Acid DerivativesAstles, Peter C. / Brown, Thomas J. / Halley, Frank / Handscombe, Caroline M. / Harris, Neil V. / Majid, Tahir N. / McCarthy, Clive / McLay, Iain M. / Morley, Andrew / Porter, Barry et al. | 2000
- 911
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Articles - Inhibition of Grb2 SH2 Domain Binding by Non-Phosphate-Containing Ligands. 2. 4-(2-Malonyl)phenylalanine as a Potent Phosphotyrosyl MimeticGao, Yang et al. | 2000
- 911
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Inhibition of Grb2 SH2 Domain Binding by Non-Phosphate-Containing Ligands. 2. 4-(2-Malonyl)phenylalanine as a Potent Phosphotyrosyl Mimetic †Gao, Yang / Luo, Juliet / Yao, Zhu-Jun / Guo, Ribo / Zou, Hong / Kelley, James / Voigt, Johannes H. / Yang, Dajun / Burke, Terrence R. et al. | 2000
- 921
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Articles - Conformationally Constrained Analogues of Diacylglycerol (DAG). 16. How Much Structural Complexity Is Necessary for Recognition and High Binding Affinity to Protein Kinase C?Nacro, Kassoum et al. | 2000
- 921
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Conformationally Constrained Analogues of Diacylglycerol (DAG). 16. How Much Structural Complexity Is Necessary for Recognition and High Binding Affinity to Protein Kinase C?Nacro, Kassoum / Bienfait, Bruno / Lee, Jeewoo / Han, Kee-Chung / Kang, Ji-Hye / Benzaria, Samira / Lewin, Nancy E. / Bhattacharyya, Dipak K. / Blumberg, Peter M. / Marquez, Victor E. et al. | 2000
- 945
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Articles - Design and Synthesis of 13,14-Dihydro Prostaglandin F1a Analogues as Potent and Selective Ligands for the Human FP ReceptorWang, Yili et al. | 2000
- 945
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Design and Synthesis of 13,14-Dihydro Prostaglandin F1α Analogues as Potent and Selective Ligands for the Human FP ReceptorWang, Yili / Wos, John A. / Dirr, Michelle J. / Soper, David L. / deLong, Mitchell A. / Mieling, Glen E. / De, Biswanath / Amburgey, Jack S. / Suchanek, Eric G. / Taylor, Cynthia J. et al. | 2000
- 945
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Design and Synthesis of 13,14-Dihydro Prostaglandin F~1~a~l~p~h~a Analogues as Potent and Selective Ligands for the Human FP ReceptorWang, Y. / Wos, J. A. / Dirr, M. J. / Soper, D. L. / deLong, M. A. / Mieling, G. E. / Suchanek, E. G. / Taylor, C. J. et al. | 2000
- 953
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Articles - Substituent Effects on the Antibacterial Activity of Nitrogen-Carbon-Linked (Azolylphenyl)oxazolidinones with Expanded Activity Against the Fastidious Gram-Negative Organisms Haemophilus influenzae and Moraxella catarrhalisGenin, Michael J. et al. | 2000
- 953
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Substituent Effects on the Antibacterial Activity of Nitrogen−Carbon-Linked (Azolylphenyl)oxazolidinones with Expanded Activity Against the Fastidious Gram-Negative Organisms Haemophilus i nfluenzae and Moraxella c atarrhalisGenin, Michael J. / Allwine, Debra A. / Anderson, David J. / Barbachyn, Michael R. / Emmert, D. Edward / Garmon, Stuart A. / Graber, David R. / Grega, Kevin C. / Hester, Jackson B. / Hutchinson, Douglas K. et al. | 2000
- 971
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Articles - Design, Synthesis, and Enzymatic Evaluation of Multisubstrate Analogue Inhibitors of Escherichia coli Thymidine PhosphorylaseEsteban-Gamboa, Antonio et al. | 2000
- 971
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Design, Synthesis, and Enzymatic Evaluation of Multisubstrate Analogue Inhibitors of Escherichia coli Thymidine PhosphorylaseEsteban-Gamboa, Antonio / Balzarini, Jan / Esnouf, Robert / De Clercq, Erik / Camarasa, María-José / Pérez-Pérez, María-Jesús et al. | 2000
- 984
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Synthesis of N-Substituted 4-(4-Hydroxyphenyl)piperidines, 4-(4-Hydroxybenzyl)piperidines, and (±)-3-(4-Hydroxyphenyl)pyrrolidines: Selective Antagonists at the 1a/2B NMDA Receptor SubtypeGuzikowski, Anthony P. / Tamiz, Amir P. / Acosta-Burruel, Manuel / Hong-Bae, Soo / Cai, Sui Xiong / Hawkinson, Jon E. / Keana, John F. W. / Kesten, Suzanne R. / Shipp, Christina T. / Tran, Minhtam et al. | 2000
- 984
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Articles - Synthesis of N-Substituted 4-(4-Hydroxyphenyl)piperidines, 4-(4-Hydroxybenzyl)piperidines, and ((plus-minus))-3-(4-Hydroxyphenyl)pyrrolidines: Selective Antagonists at the 1A-2B NMDA Receptor SubtypeGuzikowski, Anthony P. et al. | 2000
- 995
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Articles - New Azolidinediones as Inhibitors of Protein Tyrosine Phosphatase 1B with Antihyperglycemic PropertiesMalamas, Michael S. et al. | 2000
- 995
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New Azolidinediones as Inhibitors of Protein Tyrosine Phosphatase 1B with Antihyperglycemic PropertiesMalamas, Michael S. / Sredy, Janet / Gunawan, Iwan / Mihan, Brenda / Sawicki, Diane R. / Seestaller, Laura / Sullivan, Donald / Flam, Brenda R. et al. | 2000
- 1011
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Articles - 2-Substituted Tryptamines: Agents with Selectivity for 5-HT6 Serotonin ReceptorsGlennon, Richard A. et al. | 2000
- 1011
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2-Substituted Tryptamines: Agents with Selectivity for 5-HT6 Serotonin Receptors ‖Glennon, Richard A. / Lee, Mase / Rangisetty, Jagadeesh B. / Dukat, Malgorzata / Roth, Bryan L. / Savage, Jason E. / McBride, Ace / Rauser, Laura / Hufeisen, Sandy / Lee, David K. H. et al. | 2000
- 1019
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Articles - Monocyclic L-Nucleosides with Type 1 Cytokine-Inducing ActivityRamasamy, Kanda S. et al. | 2000
- 1019
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Monocyclic l-Nucleosides with Type 1 Cytokine-Inducing ActivityRamasamy, Kanda S. / Tam, Robert C. / Bard, Josie / Averett, Devron R. et al. | 2000
- 1029
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Brief Articles - N-Terminal Dipeptides of D(-)-Penicillamine as Sequestration Agents for AcetaldehydeCohen, Jonathan F. et al. | 2000
- 1029
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N-Terminal Dipeptides of d(−)-Penicillamine as Sequestration Agents for AcetaldehydeCohen, Jonathan F. / Elberling, James A. / DeMaster, Eugene G. / Lin, Renee C. / Nagasawa, Herbert T. et al. | 2000
- 1034
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Brief Articles - Novel 1,5-Diphenylpyrazole Nonnucleosicle HIV-1 Reverse Transcriptase Inhibitors with Enhanced Activity versus the Delavirdine-Resistant P236L Mutant: Lead Identification and SAR of 3- and 4-Substituted DerivativesGenin, Michael J. et al. | 2000
- 1034
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Novel 1,5-Diphenylpyrazole Nonnucleoside HIV-1 Reverse Transcriptase Inhibitors with Enhanced Activity versus the Delavirdine-Resistant P236L Mutant: Lead Identification and SAR of 3- and 4-Substituted DerivativesGenin, Michael J. / Biles, Carolyn / Keiser, Barb J. / Poppe, Susan M. / Swaney, Steven M. / Tarpley, W. Gary / Yagi, Yoshihiko / Romero, Donna L. et al. | 2000
- 1041
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Communications - Pyrrolidine Inhibitors of Human Cytosolic Phospholipase A2Seno, Kaoru et al. | 2000
- 1041
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Pyrrolidine Inhibitors of Human Cytosolic Phospholipase A2Seno, Kaoru / Okuno, Takayuki / Nishi, Koichi / Murakami, Yasushi / Watanabe, Fumihiko / Matsuura, Takaharu / Wada, Masaaki / Fujii, Yasuhiko / Yamada, Masaaki / Ogawa, Tomoyuki et al. | 2000
- 1045
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Communications - Design, Synthesis, and Antimicrobial Activity of 6-O-Substituted Ketolides Active against Resistant Respiratory Tract PathogensOr, Yat Sun et al. | 2000
- 1045
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Design, Synthesis, and Antimicrobial Activity of 6-O-Substituted Ketolides Active against Resistant Respiratory Tract PathogensOr, Yat Sun / Clark, Richard F. / Wang, Sanyi / Chu, Daniel T. W. / Nilius, Angela M. / Flamm, Robert K. / Mitten, Michael / Ewing, Patty / Alder, Jeff / Ma, Zhenkun et al. | 2000
- 1050
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Mapping the Melatonin Receptor. 6. Melatonin Agonists and Antagonists Derived from 6H-Isoindolo[2,1-a]indoles, 5,6-Dihydroindolo[2,1-a]isoquinolines, and 6,7-Dihydro-5H-benzo[c]azepino[2,1-a]indolesFaust, Rüdiger / Garratt, Peter J. / Jones, Rob / Yeh, Li-Kuan / Tsotinis, Andrew / Panoussopoulou, Maria / Calogeropoulou, Theodora / Teh, Muy-Teck / Sugden, David et al. | 2000
- 1050
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Articles - Mapping the Melatonin Receptor. 6. Melatonin Agonists and Antagonists Derived from 6H-Isoindolo(2,1-a)indoles, 5,6-Dihydroindolo(2,1-a)isoquinolines, and 6,7-Dihydro-5H-benzo(c)azepino(2,1-a)indolesFaust, Rüdiger et al. | 2000
- 1062
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Molecular Modeling of the Aldose Reductase-Inhibitor Complex Based on the X-ray Crystal Structure and Studies with Single-Site-Directed MutantsSingh, Suresh B. / Malamas, Michael S. / Hohman, Thomas C. / Nilakantan, Ramaswamy / Carper, Deborah A. / Kitchen, Douglas et al. | 2000
- 1062
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Articles - Molecular Modeling of the Aldose Reductase-Inhibitor Complex Based on the X-ray Crystal Structure and Studies with Single-Site-Directed MutantsSingh, Suresh B. et al. | 2000
- 1071
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Histaprodifens: Synthesis, Pharmacological in Vitro Evaluation, and Molecular Modeling of a New Class of Highly Active and Selective Histamine H1-Receptor Agonists †Elz, Sigurd / Kramer, Kai / Pertz, Heinz H. / Detert, Heiner / ter Laak, Anton M. / Kühne, Ronald / Schunack, Walter et al. | 2000
- 1071
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Articles - Histaprodifens: Synthesis, Pharmacological in Vitro Evaluation, and Molecular Modeling of a New Class of Highly Active and Selective Histamine H1-Receptor AgonistsElz, Sigurd et al. | 2000
- 1085
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Highly Selective Chiral N-Substituted 3alpha-[Bis(4'-fluorophenyl)methoxy]tropane Analogues for the Dopamine Transporter: Synthesis and Comparative Molecular Field AnalysisRobarge, M. J. / Agoston, G. E. / Izenwasser, S. / Kopajtic, T. / George, C. / Katz, J. L. / Hauck Newman, A. et al. | 2000
- 1085
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Articles - Highly Selective Chiral N-Substituted 3a-(Bis(4'-fluorophenyl)methoxyltropane Analogues for the Dopamine Transporter: Synthesis and Comparative Molecular Field AnalysisRobarge, Michael J. et al. | 2000
- 1085
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Highly Selective Chiral N-Substituted 3α-[Bis(4‘-fluorophenyl)methoxy]tropane Analogues for the Dopamine Transporter: Synthesis and Comparative Molecular Field AnalysisRobarge, Michael J. / Agoston, Gregory E. / Izenwasser, Sari / Kopajtic, Theresa / George, Clifford / Katz, Jonathan L. / Newman, Amy Hauck et al. | 2000
- 1094
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2‘,6‘-Dimethylphenoxyacetyl: A New Achiral High Affinity P3-P2 Ligand for Peptidomimetic-Based HIV Protease InhibitorsBeaulieu, Pierre L. / Anderson, Paul C. / Cameron, Dale R. / Croteau, Gilbert / Gorys, Vida / Grand-Maître, Chantal / Lamarre, Daniel / Liard, Francine / Paris, William / Plamondon, Louis et al. | 2000
- 1094
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Articles - 2',6'-Dimethylphenoxyacetyl: A New Achiral High Affinity P3-P2 Ligand for Peptidomimetic-Based HIV Protease InhibitorsBeaulieu, Pierre L. et al. | 2000
- 1109
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3D-QSAR CoMFA Study on Imidazolinergic I2 Ligands: A Significant Model through a Combined Exploration of Structural Diversity and MethodologyBaurin, Nicolas / Vangrevelinghe, Eric / Morin-Allory, Luc / Mérour, Jean-Yves / Renard, Pierre / Payard, Marc / Guillaumet, Gérald / Marot, Christophe et al. | 2000
- 1109
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Articles - 3D-QSAR CoMFA Study on Imidazolinergic I2 Ligands: A Significant Model through a Combined Exploration of Structural Diversity and MethodologyBaurin, Nicolas et al. | 2000
- 1123
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Biarylcarbamoylindolines Are Novel and Selective 5-HT2C Receptor Inverse Agonists: Identification of 5-Methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a Potential Antidepressant/Anxiolytic AgentBromidge, Steven M. / Dabbs, Steven / Davies, David T. / Davies, Susannah / Duckworth, D. Malcolm / Forbes, Ian T. / Gaster, Laramie M. / Ham, Peter / Jones, Graham E. / King, Frank D. et al. | 2000
- 1123
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Articles - Biarylcarbamoylindolines Are Novel and Selective 5-HT2C Receptor Inverse Agonists: Identification of 5-Methyl-1-((2-((2-methyl-3-pyridyl) oxy)-5-pyridyl)carbamoyl)-6-trifluoromethylindoline (SB-243213) as a Potential Antidepressant-Anxiolytic AgentBromidge, Steven M. et al. | 2000
- 1135
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Investigating Protein−Ligand Interactions with a Mutant FKBP Possessing a Designed Specificity PocketYang, Wu / Rozamus, Leonard W. / Narula, Surinder / Rollins, Carl T. / Yuan, Ruth / Andrade, Lawrence J. / Ram, Mary K. / Phillips, Thomas B. / van Schravendijk, Marie Rose / Dalgarno, David et al. | 2000
- 1135
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Articles - Investigating Protein-Ligand Interactions with a Mutant FKBP Possessing a Designed Specificity PocketYang, Wu et al. | 2000
- 1143
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Articles - Artificial Neural Network Applied to Prediction of Fluorquinolone Antibacterial Activity by Topological MethodsJaén-Oltra, José et al. | 2000
- 1143
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Artificial Neural Network Applied to Prediction of Fluorquinolone Antibacterial Activity by Topological MethodsJaén-Oltra, José / Salabert-Salvador, Ma Teresa / García-March, Francisco J. / Pérez-Giménez, Facundo / Tomás-Vert, Francisco et al. | 2000
- 1149
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5-HT Reuptake Inhibitors with 5-HT1B/1D Antagonistic Activity: A New Approach toward Efficient AntidepressantsMatzen, Lisa / van Amsterdam, Christoph / Rautenberg, Wilfried / Greiner, Hartmut E. / Harting, Jürgen / Seyfried, Christoph A. / Böttcher, Henning et al. | 2000
- 1149
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Articles - 5-HT Reuptake Inhibitors with 5-HT1B-1D Antagonistic Activity: A New Approach toward Efficient AntidepressantsMatzen, Lisa et al. | 2000
- 1158
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Articles - 1,2,4-Triazolo(4,3-a)quinoxalin-1-one: A Versatile Tool for the Synthesis of Potent and Selective Adenosine Receptor AntagonistsColotta, Vittoria et al. | 2000
- 1158
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1,2,4-Triazolo[4,3-a]quinoxalin-1-one: A Versatile Tool for the Synthesis of Potent and Selective Adenosine Receptor AntagonistsColotta, Vittoria / Catarzi, Daniela / Varano, Flavia / Cecchi, Lucia / Filacchioni, Guido / Martini, Claudia / Trincavelli, Letizia / Lucacchini, Antonio et al. | 2000
- 1158
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1,2,4-Triazolo[4,3-alpha]quinoxalin-l-one: A Versatile Tool for the Synthesis of Potent and Selective Adenosine Receptor AntagonistsColotta, V. / Catarzi, D. / Varano, F. / Cecchi, L. / Filacchioni, G. / Martini, C. / Trincavelli, L. / Lucacchini, A. et al. | 2000
- 1165
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Anilide Derivatives of an 8-Phenylxanthine Carboxylic Congener Are Highly Potent and Selective Antagonists at Human A2B Adenosine ReceptorsKim, Yong-Chul / Ji, Xiao-duo / Melman, Neli / Linden, Joel / Jacobson, Kenneth A. et al. | 2000
- 1165
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Articles - Anilide Derivatives of an 8-Phenylxanthine Carboxylic Congener Are Highly Potent and Selective Antagonists at Human A2B Adenosine ReceptorsKim, Yong-Chul et al. | 2000
- 1173
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Articles - SH2-Directed Ligands of the Lck Tyrosine KinaseLee, Tae Ryong et al. | 2000
- 1173
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SH2-Directed Ligands of the Lck Tyrosine KinaseLee, Tae Ryong / Lawrence, David S. et al. | 2000
- 1180
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Doubly Homologated Dihalovinyl and Acetylene Analogues of Adenosine: Synthesis, Interaction with S-Adenosyl-l-homocysteine Hydrolase, and Antiviral and Cytostatic EffectsWnuk, Stanislaw F. / Valdez, Carlos A. / Khan, Jahanzeb / Moutinho, Priscilla / Robins, Morris J. / Yang, Xiaoda / Borchardt, Ronald T. / Balzarini, Jan / De Clercq, Erik et al. | 2000
- 1180
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Articles - Doubly Homologated Dihalovinyl and Acetylene Analogues of Adenosine: Synthesis, Interaction with S-Adenosyl-L-homocysteine Hydrolase, and Antiviral and Cytostatic EffectsWnuk, Stanislaw F. et al. | 2000
- 1187
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Design and SAR of Novel Potassium Channel Openers Targeted for Urge Urinary Incontinence. 1. N-Cyanoguanidine Bioisosteres Possessing in Vivo Bladder SelectivityButera, John A. / Antane, Madelene M. / Antane, Schuyler A. / Argentieri, Thomas M. / Freeden, Chris / Graceffa, Russell F. / Hirth, Bradford H. / Jenkins, Douglas / Lennox, Joseph R. / Matelan, Edward et al. | 2000
- 1187
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Articles - Design and SAR of Novel Potassium Channel Openers Targeted for Urge Urinary Incontinence. 1. N-Cyanoguanidine Bioisosteres Possessing in Vivo Bladder SelectivityButera, John A. et al. | 2000
- 1203
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Design and SAR of Novel Potassium Channel Openers Targeted for Urge Urinary Incontinenece. 2. Selective and Potent Benzylamino CyclobutenedionesGilbert, A. M. / Antane, M. M. / Argentieri, T. M. / Butera, J. A. / Francisco, G. D. / Freeden, C. / Gundersen, E. G. / Graceffa, R. F. / Herbst, D. / Hirth, B. H. et al. | 2000
- 1203
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Design and SAR of Novel Potassium Channel Openers Targeted for Urge Urinary Incontinence. 2. Selective and Potent Benzylamino CyclobutenedionesGilbert, Adam M. / Antane, Madelene M. / Argentieri, Thomas M. / Butera, John A. / Francisco, Gerardo D. / Freeden, Chris / Gundersen, Eric G. / Graceffa, Russell F. / Herbst, David / Hirth, Bradford H. et al. | 2000
- 1203
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Articles - Design and SAR of Novel Potassium Channel Openers Targeted for Urge Urinary Incontinence. 2. Selective and Potent Benzylamino CyclobutenedionesGilbert, Adam M. et al. | 2000
- 1215
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Further SAR Studies of Piperidine-Based Analogues of Cocaine. 2. Potent Dopamine and Serotonin Reuptake InhibitorsTamiz, Amir P. / Zhang, Jianrong / Flippen-Anderson, Judith L. / Zhang, Mei / Johnson, Kenneth M. / Deschaux, Olivier / Tella, Srihari / Kozikowski, Alan P. et al. | 2000
- 1215
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Articles - Further SAR Studies of Piperidine-Based Analogues of Cocaine. 2. Potent Dopamine and Serotonin Reuptake InhibitorsTamiz, Amir P. et al. | 2000
- 1223
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Articles - Novel and Selective Calcitonin-Inducing AgentsGilbert, Adam M. et al. | 2000
- 1223
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Novel and Selective Calcitonin-Inducing AgentsGilbert, Adam M. / Caltabiano, Stephen / Roberts, Denise / Sum, Sam F. W. / Francisco, Gerardo D. / Lim, Kitae / Asselin, Magda / Ellingboe, John W. / Kharode, Yogendra / Cannistraci, Anna et al. | 2000
- 1234
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Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble ProdrugsHale, Jeffrey J. / Mills, Sander G. / MacCoss, Malcolm / Dorn, Conrad P. / Finke, Paul E. / Budhu, Richard J. / Reamer, Robert A. / Huskey, Su-Er W. / Luffer-Atlas, Debra / Dean, Brian J. et al. | 2000
- 1234
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Articles - Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble ProdrugsHale, Jeffrey J. et al. | 2000
- 1242
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Brief Articles - Active Conformations of Neotame and Other High-Potency SweetenersWalters, D.Eric et al. | 2000
- 1242
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Active Conformations of Neotame and Other High-Potency SweetenersWalters, D. Eric / Prakash, Indra / Desai, Nitin et al. | 2000
- 1246
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Brief Articles - Methyl-Substituted Dispiro-1,2,4,5-tetraoxanes: Correlations of Structural Studies with Antimalarial ActivityMcCullough, Kevin J. et al. | 2000
- 1246
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Methyl-Substituted Dispiro-1,2,4,5-tetraoxanes: Correlations of Structural Studies with Antimalarial ActivityMcCullough, Kevin J. / Wood, James K. / Bhattacharjee, Apurba K. / Dong, Yuxiang / Kyle, Dennis E. / Milhous, Wilbur K. / Vennerstrom, Jonathan L. et al. | 2000
- 1250
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Additions and Corrections - Conformationally Constrained Butyrophenones with Mixed Dopaminergic (D2) and Serotoninergic (5-HT2A, 5-HT2C) Affinities: Synthesis, Pharmacology, SD-QSAR, and Molecular Modeling of (Aminoalkyl)benzo- and -thienocycloalkanones as Putative Atypical AntipsychoticsRaviña, Enrique et al. | 2000
- 1250
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Conformationally Constrained Butyrophenones with Mixed Dopaminergic (D2) and Serotoninergic (5-HT2A, 5-HT2C) Affinities: Synthesis, Pharmacology, 3D-QSAR, and Molecular Modeling of (Aminoalkyl)benzo- and -thienocycloalkanones as Putative Atypical Antipsychotics.Raviña, Enrique / Negreira, Jesús / Cid, José / Masaguer, Christian F. / Rosa, Elizabeth / Rivas, M. Emilia / Fontenla, José A. / Loza, M. Isabel / Tristán, Helena / Cadavid, M. Isabel et al. | 2000
- 1251
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Isosteric Replacement of Acidic with Neutral Residues in Extracellular Loop-2 of the κ-Opioid Receptor Does Not Affect Dynorphin A(1−13) Affinity and FunctionFerguson, David M. / Kramer, Stacy / Metzger, Thomas G. / Law, Ping Y. / Portoghese, Philip S. et al. | 2000
- 1251
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Communications - Isosteric Replacement of Acidic with Neutral Residues in Extracellular Loop-2 of the k-Opioid Receptor Does Not Affect Dynorphin A(1-13) Affinity and FunctionFerguson, David M. et al. | 2000
- 1251
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Isosteric Replacement of Acidic with Neutral Residues in Extracellular Loop-2 of the kappa-Opioid Receptor Does Not Affect Dynorphin A(1-13) Affinity and FunctionFerguson, D. M. / Kramer, S. / Metzger, T. G. / Law, P. Y. / Portoghese, P. S. et al. | 2000
- 1253
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Communications - A Novel Macromolecular Prodrug Concept Exploiting Endogenous Serum Albumin as a Drug Carrier for Cancer ChemotherapyKratz, Felix et al. | 2000
- 1253
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A Novel Macromolecular Prodrug Concept Exploiting Endogenous Serum Albumin as a Drug Carrier for Cancer ChemotherapyKratz, Felix / Müller-Driver, Ralph / Hofmann, Inga / Drevs, Joachim / Unger, Clemens et al. | 2000
- 1257
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N-3-Substituted Imidazoquinazolinones: Potent and Selective PDE5 Inhibitors as Potential Agents for Treatment of Erectile DysfunctionRotella, David P. / Sun, Zhong / Zhu, Yeheng / Krupinski, John / Pongrac, Ronald / Seliger, Laurie / Normandin, Diane / Macor, John E. et al. | 2000
- 1257
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Expedited Articles - N-3-Substituted Imidazoquinazolinones: Potent and Selective PDE5 Inhibitors as Potential Agents for Treatment of Erectile DysfunctionRotella, David P. et al. | 2000
- 1264
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Articles - Synthesis, Conformational Analysis, and Biological Activity of C-Thioribonucleosides Related to TiazofurinFranchetti, Palmarisa et al. | 2000
- 1264
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Synthesis, Conformational Analysis, and Biological Activity of C-Thioribonucleosides Related to TiazofurinFranchetti, Palmarisa / Marchetti, Stefano / Cappellacci, Loredana / Jayaram, Hiremagalur N. / Yalowitz, Joel Aaron / Goldstein, Barry M. / Barascut, Jean-Louis / Dukhan, David / Imbach, Jean-Louis / Grifantini, Mario et al. | 2000
- 1271
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Conformational Selection of Inhibitors and Substrates by Proteolytic Enzymes: Implications for Drug Design and Polypeptide ProcessingFairlie, David P. / Tyndall, Joel D. A. / Reid, Robert C. / Wong, Allan K. / Abbenante, Giovanni / Scanlon, Martin J. / March, Darren R. / Bergman, Douglas A. / Chai, Christina L. L. / Burkett, Brendan A. et al. | 2000
- 1271
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Articles - Conformational Selection of Inhibitors and Substrates by Proteolytic Enzymes: Implications for Drug Design and Polypeptide ProcessingFairlie, David P. et al. | 2000
- 1282
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Cyclin-Dependent Kinase Inhibition by New C-2 Alkynylated Purine Derivatives and Molecular Structure of a CDK2−Inhibitor ComplexLegraverend, Michel / Tunnah, Paul / Noble, Martin / Ducrot, Pierre / Ludwig, Odile / Grierson, David S. / Leost, Maryse / Meijer, Laurent / Endicott, Jane et al. | 2000
- 1282
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Articles - Cyclin-Dependent Kinase Inhibition by New C-2 Alkynylated Purine Derivatives and Molecular Structure of a CDK2-Inhibitor ComplexLegraverend, Michel et al. | 2000
- 1293
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Novel Benzofuran and Benzothiophene Biphenyls as Inhibitors of Protein Tyrosine Phosphatase 1B with Antihyperglycemic PropertiesMalamas, Michael S. / Sredy, Janet / Moxham, Christopher / Katz, Alan / Xu, Weixin / McDevitt, Robert / Adebayo, Folake O. / Sawicki, Diane R. / Seestaller, Laura / Sullivan, Donald et al. | 2000
- 1293
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Articles - Novel Benzofuran and Benzothiophene Biphenyls as Inhibitors of Protein Tyrosine Phosphatase 1B with Antihyperglycemic PropertiesMalamas, Michael S. et al. | 2000
- 1311
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Synthesis and Anticonvulsant and Neurotoxic Properties of Substituted N-Phenyl Derivatives of the Phthalimide PharmacophoreVamecq, Joseph / Bac, Pierre / Herrenknecht, Christine / Maurois, Pierre / Delcourt, Philippe / Stables, James P. et al. | 2000
- 1311
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Articles - Synthesis and Anticonvulsant and Neurotoxic Properties of Substituted N-Phenyl Derivatives of the Phthalimide PharmacophoreVamecq, Joseph et al. | 2000
- 1320
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Statistical Molecular Design of Building Blocks for Combinatorial ChemistryLinusson, Anna / Gottfries, Johan / Lindgren, Fredrik / Wold, Svante et al. | 2000
- 1320
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Articles - Statistical Molecular Design of Building Blocks for Combinatorial ChemistryLinusson, Anna et al. | 2000
- 1329
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High-Affinity, Non-Peptide Agonists for the ORL1 (Orphanin FQ/Nociceptin) ReceptorRöver, Stephan / Adam, Geo / Cesura, Andrea M. / Galley, Guido / Jenck, François / Monsma,, Frederick J. / Wichmann, Jürgen / Dautzenberg, Frank M. et al. | 2000
- 1329
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Articles - High-Affinity, Non-Peptide Agonists for the ORL1 (Orphanin FQ-Nociceptin) ReceptorRöver, Stephan et al. | 2000
- 1339
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Derivatives of (R)-1,11-Methyleneaporphine: Synthesis, Structure, and Interactions with G-Protein Coupled ReceptorsLinnanen, Tero / Brisander, Magnus / Unelius, Lena / Sundholm, Göran / Hacksell, Uli / Johansson, Anette M. et al. | 2000
- 1339
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Articles - Derivatives of (R)-1,11-Methyleneaporphine: Synthesis, Structure, and Interactions with G-Protein Coupled ReceptorsLinnanen, Tero et al. | 2000
- 1350
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Bis(phenazine-1-carboxamides): Structure−Activity Relationships for a New Class of Dual Topoisomerase I/II-Directed Anticancer DrugsSpicer, Julie A. / Gamage, Swarna A. / Rewcastle, Gordon W. / Finlay, Graeme J. / Bridewell, David J. A. / Baguley, Bruce C. / Denny, William A. et al. | 2000
- 1350
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Articles - Bis(phenazine-1-carboxamides): Structure-Activity Relationships for a New Class of Dual, Topoisomerase I-II-Directed Anticancer DrugsSpicer, Julie A. et al. | 2000
- 1359
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Deltorphin II Analogues with 6-Hydroxy-2-aminotetralin-2-carboxylic Acid in Position 1Darula, Zsuzsanna / Kövér, Katalin E. / Monory, Krisztina / Borsodi, Anna / Makó, Éva / Rónai, András / Tourwé, Dirk / Péter, Antal / Tóth, Géza et al. | 2000
- 1359
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Articles - Deltorphin II Analogues with 6-Hydroxy-2-aminotetralin-2-carboxylic Acid in Position 1Darula, Zsuzsanna et al. | 2000
- 1367
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Lipopolycationic Telomers for Gene Transfer: Synthesis and Evaluation of Their in Vitro Transfection EfficiencyVerderone, Géraldine / Van Craynest, Nathalie / Boussif, Otmane / Santaella, Catherine / Bischoff, Rainer / Kolbe, Hanno V. J. / Vierling, Pierre et al. | 2000
- 1367
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Articles - Lipopolycationic Telomers for Gene Transfer: Synthesis and Evaluation of Their in Vitro Transfection EfficiencyVerderone, Géraldine et al. | 2000
- 1380
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Articles - Tyrosine Kinase Inhibitors. 17. Irreversible Inhibitors of the Epidermal Growth Factor Receptor: 4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido(3,2-d)pyrimidine-6-acrylamides Bearing Additional Solubilizing FunctionsSmaill, Jeff B. et al. | 2000
- 1380
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Tyrosine Kinase Inhibitors. 17. Irreversible Inhibitors of the Epidermal Growth Factor Receptor: 4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides Bearing Additional Solubilizing FunctionsSmaill, Jeff B. / Rewcastle, Gordon W. / Loo, Joseph A. / Greis, Kenneth D. / Chan, O. Helen / Reyner, Eric L. / Lipka, Elke / Showalter, H. D. Hollis / Vincent, Patrick W. / Elliott, William L. et al. | 2000
- 1398
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Phosphinic Derivatives as New Dual Enkephalin-Degrading Enzyme Inhibitors: Synthesis, Biological Properties, and Antinociceptive ActivitiesChen, Huixiong / Noble, Florence / Mothé, Aurélie / Meudal, Hervé / Coric, Pascale / Danascimento, Sophie / Roques, Bernard P. / George, Pascal / Fournié-Zaluski, Marie-Claude et al. | 2000
- 1398
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Articles - Phosphinic Derivatives as New Dual Enkephalin-Degrading Enzyme Inhibitors: Synthesis, Biological Properties, and Antinociceptive ActivitiesChen, Huixiong et al. | 2000
- 1409
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Synthesis and Oral Antitumor Activity of Tetrakis(carboxylato)platinum(IV) ComplexesLee, Young-A / Lee, Sung Sil / Kim, Kwan Mook / Lee, Chong Ock / Sohn, Youn Soo et al. | 2000
- 1409
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Brief Articles - Synthesis and Oral Antitumor Activity of Tetrakis(carboxylato)platinum(IV) ComplexesLee, Young-A. et al. | 2000
- 1413
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Inhibition of Protein Kinase Cα by Dequalinium Analogues: Dependence on Linker Length and GeometryQin, Donghui / Sullivan, Regina / Berkowitz, William F. / Bittman, Robert / Rotenberg, Susan A. et al. | 2000
- 1413
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Brief Articles - Inhibition of Protein Kinase Ca by Dequalinium Analogues: Dependence on Linker Length and GeometryQin, Donghui et al. | 2000
- 1413
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Inhibition of Protein Kinase Calpha by Dequalinium Analogues: Dependence on Linker Length and GeometryQin, D. / Sullivan, R. / Berkowitz, W. F. / Bittman, R. / Rotenberg, S. A. et al. | 2000
- 1418
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Brief Articles - Protection against Oxidative Damage by Iron Chelators: Effect of Lipophilic Analogues and Prodrugs of N,N'-Bis(3,4,5-trimethoxybenzyl)-ethylenediamine-N,N'-diacetic Acid (OR10141)Galey, Jean-Baptiste et al. | 2000
- 1418
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Protection against Oxidative Damage by Iron Chelators: Effect of Lipophilic Analogues and Prodrugs of N,N‘-Bis(3,4,5-trimethoxybenzyl)ethylenediamine- N,N‘-diacetic Acid (OR10141)Galey, Jean-Baptiste / Destrée, Odile / Dumats, Jacqueline / Génard, Sylvie / Tachon, Pierre et al. | 2000
- 1422
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Book Reviews - Books of Interest| 2000
- 1423
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Additions and Corrections - a2 Adrenoceptor Agonists as Potential Analgesic Agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene as a High-Affinity Ligand for the a2D Adrenergic ReceptorRoss, Tina M. et al. | 2000
- 1427
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GABA-Activated Ligand Gated Ion Channels: Medicinal Chemistry and Molecular BiologyChebib, Mary / Johnston, Graham A. R. et al. | 2000
- 1427
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Perspectives - GABA-Activated Ligand Gated Ion Channels: Medicinal Chemistry and Molecular BiologyChebib, Mary et al. | 2000
- 1448
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A Study of the Relationship between Biological Activity and Prolyl Amide Isomer Geometry in Oxytocin Using 5-tert-Butylproline To Augment the Cys6-Pro7 Amide Cis-Isomer PopulationBélec, Laurent / Slaninova, Jirina / Lubell, William D. et al. | 2000
- 1448
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Articles - A Study of the Relationship between Biological Activity and Prolyl Amide Isomer Geometry in Oxytocin Using 5-tert-Butylproline To Augment the Cys6-Pro7 Amide Cis-Isomer PopulationBélec, Laurent et al. | 2000
- 1456
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3-Alkylamino-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-Dioxides Structurally Related to Diazoxide and Pinacidil as Potassium Channel Openers Acting on Vascular Smooth Muscle Cells: Design, Synthesis, and Pharmacological EvaluationPirotte, Bernard / Ouedraogo, Raogo / de Tullio, Pascal / Khelili, Smail / Somers, Fabian / Boverie, Stéphane / Dupont, Léon / Fontaine, Jeanine / Damas, Jacques / Lebrun, Philippe et al. | 2000
- 1456
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Articles - 3-Alkylamino-4H-pyrido(2,3-e)-1,2,4-thiadiazine 1,1-Dioxides Structurally Related to Diazoxide and Pinacidil as Potassium Channel Openers Acting on Vascular Smooth Muscle Cells: Design, Synthesis, and Pharmacological EvaluationPirotte, Bernard et al. | 2000
- 1467
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Articles - Improving the Oral Bioavailability of the Iron Chelator HBED by Breaking the Symmetry of the Intramolecular H-Bond NetworkFaller, Bernard et al. | 2000
- 1467
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Improving the Oral Bioavailability of the Iron Chelator HBED by Breaking the Symmetry of the Intramolecular H-Bond Network †Faller, Bernard / Spanka, Carsten / Sergejew, Thomas / Tschinke, Vincenzo et al. | 2000
- 1476
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Articles - Study on Selectin Blocker. 8. Lead Discovery of a Non-Sugar Antagonist Using a 3D-Pharmacophore ModelHiramatsu, Yasuyuki et al. | 2000
- 1476
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Study on Selectin Blocker. 8. Lead Discovery of a Non-Sugar Antagonist Using a 3D-Pharmacophore ModelHiramatsu, Yasuyuki / Tsukida, Takahiro / Nakai, Yoshiyuki / Inoue, Yoshimasa / Kondo, Hirosato et al. | 2000
- 1476
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Study on Selection Blocker.8. Lead Discovery of a Non-Sugar Antagonist Using a 3D-Pharmacophore ModelHiramatsu, Y. / Tsukida, T. / Nakai, Y. / Inoue, Y. / Kondo, H. et al. | 2000
- 1484
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Synthesis and Evaluation of Several New (2-Chloroethyl)nitrosocarbamates as Potential Anticancer AgentsReynolds, Robert C. / Tiwari, Anita / Harwell, Joyce E. / Gordon, Deborah G. / Garrett, Beverly D. / Gilbert, Karen S. / Schmid, Steven M. / Waud, William R. / Struck, Robert F. et al. | 2000
- 1484
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Articles - Synthesis and Evaluation of Several New (2-Chloroethyl)nitrosocarbamates as Potential Anticancer AgentsReynolds, Robert C. et al. | 2000
- 1489
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Synthesis and in Vitro Evaluation of Novel Morpholinyl- and Methylpiperazinylacyloxyalkyl Prodrugs of 2-(6-Methoxy-2-naphthyl)propionic Acid (Naproxen) for Topical Drug DeliveryRautio, Jarkko / Nevalainen, Tapio / Taipale, Hannu / Vepsäläinen, Jouko / Gynther, Jukka / Laine, Krista / Järvinen, Tomi et al. | 2000
- 1489
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Articles - Synthesis and in Vitro Evaluation of Novel Morpholinyl- and Methylpiperazinylacyl- oxyalkyl Prodrugs of 2-(6-Methoxy-2-naphthyl)-propionic Acid (Naproxen) for Topical Drug DeliveryRautio, Jarkko et al. | 2000
- 1495
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AMP Deaminase Inhibitors. 2. Initial Discovery of a Non-Nucleotide Transition-State Inhibitor SeriesBookser, Brett C. / Kasibhatla, Srinivas Rao / Appleman, James R. / Erion, Mark D. et al. | 2000
- 1495
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Articles - AMP Deaminase Inhibitors. 2. Initial Discovery of a Non-Nucleotide Transition-State Inhibitor SeriesBookser, Brett C. et al. | 2000
- 1508
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AMP Deaminase Inhibitors. 3. SAR of 3-(Carboxyarylalkyl)coformycin Aglycon AnaloguesKasibhatla, Srinivas Rao / Bookser, Brett C. / Probst, Gary / Appleman, James R. / Erion, Mark D. et al. | 2000
- 1508
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Articles - AMP Deaminase Inhibitors. 3. SAR of 3-(Carboxyarylalkyl)coformycin Aglycon AnaloguesKasibhatla, Srinivas Rao et al. | 2000
- 1519
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AMP Deaminase Inhibitors. 4. Further N3-Substituted Coformycin Aglycon Analogues: N3-Alkylmalonates as Ribose 5‘-Monophosphate MimeticsBookser, Brett C. / Kasibhatla, Srinivas Rao / Erion, Mark D. et al. | 2000
- 1519
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Articles - AMP Deaminase Inhibitors. 4. Further N3-Substituted Coformycin Aglycon Analogues: N3-Alkylmalonates as Ribose 5'-Monophosphate MimeticsBookser, Brett C. et al. | 2000
- 1525
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Articles - Soft Drugs. 12. Design, Synthesis, and Evaluation of Soft Bufuralol AnaloguesHwang, Sung-Kwan et al. | 2000
- 1525
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Soft Drugs. 12. Design, Synthesis, and Evaluation of Soft Bufuralol AnaloguesHwang, Sung-Kwan / Juhasz, Attila / Yoon, Sung-Hwa / Bodor, Nicholas et al. | 2000
- 1533
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Articles - Structure-Activity Relationships and Binding Mode of Styrylquinolines as Potent Inhibitors of HIV-1 Integrase and Replication of HIV-1 in Cell CultureZouhiri, Fatima et al. | 2000
- 1533
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Structure−Activity Relationships and Binding Mode of Styrylquinolines as Potent Inhibitors of HIV-1 Integrase and Replication of HIV-1 in Cell CultureZouhiri, Fatima / Mouscadet, Jean-François / Mekouar, Khalid / Desmaële, Didier / Savouré, Delphine / Leh, Hervé / Subra, Frédéric / Le Bret, Marc / Auclair, Christian / d'Angelo, Jean et al. | 2000
- 1541
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Articles - Synthesis and Preliminary Biological Evaluations of CC-1065 Analogues: Effects of Different Linkers and Terminal Amides on Biological ActivityWang, Yuqiang et al. | 2000
- 1541
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Synthesis and Preliminary Biological Evaluations of CC-1065 Analogues: Effects of Different Linkers and Terminal Amides on Biological ActivityWang, Yuqiang / Yuan, Huiling / Ye, Wenqing / Wright, Susan C. / Wang, Hong / Larrick, James W. et al. | 2000
- 1550
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Articles - Structural Studies on Bioactive Compounds. 32. Oxidation of Tyrphostin Protein Tyrosine Kinase Inhibitors with Hypervalent Iodine ReagentsWells, Geoffrey et al. | 2000
- 1550
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Structural Studies on Bioactive Compounds. 32. Oxidation of Tyrphostin Protein Tyrosine Kinase Inhibitors with Hypervalent Iodine ReagentsWells, Geoffrey / Seaton, Angela / Stevens, Malcolm F. G. et al. | 2000
- 1550
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Structural Studies on Bioactive Compounds.32. Oxidation of Tyrphostin Tyrosine Kinase Inhibitors with Hypervalent Iodine ReagentsWells, G. / Seaton, A. / Stevens, M. F. et al. | 2000
- 1563
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Articles - Antitumor Polyeyclic Acridines. 7. Synthesis and Biological Properties of DNA Affinic Tetra- and Pentacyclic AcridinesStanslas, Johnson et al. | 2000
- 1563
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Antitumor Polycyclic Acridines. 7. Synthesis and Biological Properties of DNA Affinic Tetra- and Pentacyclic AcridinesStanslas, Johnson / Hagan, Damien J. / Ellis, Michael J. / Turner, Claire / Carmichael, James / Ward, Wynne / Hammonds, Timothy R. / Stevens, Malcolm F. G. et al. | 2000
- 1573
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Binding of Norbinaltorphimine (norBNI) Congeners to Wild-Type and Mutant Mu and Kappa Opioid Receptors: Molecular Recognition Loci for the Pharmacophore and Address Components of Kappa AntagonistsLarson, Dennis L. / Jones, Robert M. / Hjorth, Siv A. / Schwartz, Thue W. / Portoghese, Philip S. et al. | 2000
- 1573
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Articles - Binding of Norbinaltorphimine (norBNI) Congeners to Wild-Type and Mutant Mu and Kappa Opioid Receptors: Molecular Recognition Loci for the Pharmacophore and Address Components of Kappa AntagonistsLarson, Dennis L. et al. | 2000
- 1577
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Synthesis and Evaluation of Tryprostatin B and Demethoxyfumitremorgin C AnaloguesWang, Haishan / Usui, Takeo / Osada, Hiroyuki / Ganesan, A. et al. | 2000
- 1577
-
Articles - Synthesis and Evaluation of Tryprostatin B and Demethoxyfumitremorgin C AnaloguesWang, Haishan et al. | 2000
- 1586
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Structure-Activity Studies for a Novel Series of Tricyclic Substituted Hexahydrobenz[e]-isoindole alpha~1~A Adrenoceptor Antagonists as Potential Agents for the Symptomatic Treatment of Benign Prostatic Hyperplasia (BPH)Meyer, M. D. / Altenbach, R. J. / Basha, F. Z. / Carroll, W. A. / Condon, S. / Elmore, S. W. / Kerwin, J. F. / Sippy, K. B. / Tietje, K. / Wendt, M. D. et al. | 2000
- 1586
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Articles - Structure-Activity Studies for a Novel Series of Tricyclic Substituted Hexahydrobenz(el- isoindole a1A Adrenoceptor Antagonists as Potential Agents for the Symptomatic Treatment of Benign Prostatic Hyperplasia (BPH)Meyer, Michael D. et al. | 2000
- 1586
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Structure−Activity Studies for a Novel Series of Tricyclic Substituted Hexahydrobenz[e]isoindole α1A Adrenoceptor Antagonists as Potential Agents for the Symptomatic Treatment of Benign Prostatic Hyperplasia (BPH)Meyer, Michael D. / Altenbach, Robert J. / Basha, Fatima Z. / Carroll, William A. / Condon, Stephen / Elmore, Steven W. / Kerwin, James F. / Sippy, Kevin B. / Tietje, Karin / Wendt, Michael D. et al. | 2000
- 1604
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Synthesis, Spectroscopy, and Cytotoxicity of Glycosylated Acetogenin Derivatives as Promising Molecules for Cancer TherapyQueiroz, Emerson F. / Roblot, François / Duret, Philippe / Figadère, Bruno / Gouyette, Alain / Laprévote, Olivier / Serani, Laurent / Hocquemiller, Reynald et al. | 2000
- 1604
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Articles - Synthesis, Spectroscopy, and Cytotoxicity of Glycosylated Acetogenin Derivatives as Promising Molecules for Cancer TherapyQueiroz, Emerson F. et al. | 2000
- 1611
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Articles - Syntheses of (R)- and (8)-2- and 6-Fluoronorepinephrine and (R)- and (S)-2- and 6-Fluoroepinephrine: Effect of Stereochemistry on Fluorine-Induced Adrenergic SelectivitiesLu, Shou-fu et al. | 2000