The First Potent Inhibitors for Human Glutaminyl Cyclase: Synthesis and Structure-Activity Relationship (Englisch)
- Neue Suche nach: Buchholz, M.
- Neue Suche nach: Buchholz, M.
- Neue Suche nach: Heiser, U.
- Neue Suche nach: Schilling, S.
- Neue Suche nach: Niestroj, A.J.
- Neue Suche nach: Zunkel, K.
- Neue Suche nach: Demuth, H.-U.
In:
Journal of medicinal chemistry
;
49
, 2
; 664-677
;
2006
-
ISSN:
- Aufsatz (Zeitschrift) / Print
-
Titel:The First Potent Inhibitors for Human Glutaminyl Cyclase: Synthesis and Structure-Activity Relationship
-
Beteiligte:Buchholz, M. ( Autor:in ) / Heiser, U. / Schilling, S. / Niestroj, A.J. / Zunkel, K. / Demuth, H.-U.
-
Erschienen in:Journal of medicinal chemistry ; 49, 2 ; 664-677
-
Verlag:
- Neue Suche nach: American Chemical Society
-
Erscheinungsort:Easton, Pa.
-
Erscheinungsdatum:2006
-
ISSN:
-
ZDBID:
-
Medientyp:Aufsatz (Zeitschrift)
-
Format:Print
-
Sprache:Englisch
- Neue Suche nach: 770/4230
- Neue Suche nach: 44.42 / 44.42
- Weitere Informationen zu Basisklassifikation
-
Schlagwörter:
-
Klassifikation:
-
Datenquelle:
Inhaltsverzeichnis – Band 49, Ausgabe 2
Zeige alle Jahrgänge und Ausgaben
Die Inhaltsverzeichnisse werden automatisch erzeugt und basieren auf den im Index des TIB-Portals verfügbaren Einzelnachweisen der enthaltenen Beiträge. Die Anzeige der Inhaltsverzeichnisse kann daher unvollständig oder lückenhaft sein.
- 441
-
Potent and Selective Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors. 1. 4-(4-Bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-onesWallace, Eli M. / Lyssikatos, Joseph / Blake, James F. / Seo, Jeongbeob / Yang, Hong Woon / Yeh, Tammie C. / Perrier, Michele / Jarski, Heidi / Marsh, Vivienne / Poch, Gregory et al. | 2006
- 445
-
HIV Integrase Inhibitors with Nucleobase Scaffolds: Discovery of a Highly Potent Anti-HIV AgentNair, Vasu / Chi, Guochen / Ptak, Roger / Neamati, Nouri et al. | 2006
- 448
-
A Minimalist Design Approach to Antimicrobial Agents Based on a Thionin TemplateVila-Perelló, Miquel / Tognon, Sabrina / Sánchez-Vallet, Andrea / García-Olmedo, Francisco / Molina, Antonio / Andreu, David et al. | 2006
- 452
-
Novel Potential Anticancer Naphthyl Phosphoramidates of BVdU: Separation of Diastereoisomers and Assignment of the Absolute Configuration of the Phosphorus CenterCongiatu, Costantino / Brancale, Andrea / Mason, Malcolm D. / Jiang, Wen G. / McGuigan, Christopher et al. | 2006
- 456
-
Selective Inhibition of Matrix Metalloproteinase Isozymes and in Vivo Protection against Emphysema by Substituted γ-Keto Carboxylic AcidsMa, Dawei / Jiang, Yongwen / Chen, Fangping / Gong, Li-kun / Ding, Ke / Xu, Yong / Wang, Renxiao / Ge, Aihua / Ren, Jin / Li, Jingya et al. | 2006
- 456
-
Selective Inhibition of Matrix Metalloproteinase Isozymes and in Vivo Protection against Emphysema by Substituted gamma-Keto Carboxylic AcidsMa, D. / Jiang, Y. / Chen, F. / Li-kun / Gong / Ding, K. / Xu, Y. / Wang, R. / Ge, A. / Ren, J. et al. | 2006
- 459
-
Novel Tacrine−Melatonin Hybrids as Dual-Acting Drugs for Alzheimer Disease, with Improved Acetylcholinesterase Inhibitory and Antioxidant PropertiesRodríguez-Franco, María Isabel / Fernández-Bachiller, María Isabel / Pérez, Concepción / Hernández-Ledesma, Blanca / Bartolomé, Begoña et al. | 2006
- 463
-
Targeting FtsZ for Antituberculosis Drug Discovery: Noncytotoxic Taxanes as Novel Antituberculosis AgentsHuang, Qing / Kirikae, Fumiko / Kirikae, Teruo / Pepe, Antonella / Amin, Amol / Respicio, Laurel / Slayden, Richard A. / Tonge, Peter J. / Ojima, Iwao et al. | 2006
- 467
-
Rapid Synthesis of Triazole-Modified Resveratrol Analogues via Click ChemistryPagliai, Francesca / Pirali, Tracey / Del Grosso, Erika / Di Brisco, Riccardo / Tron, Gian Cesare / Sorba, Giovanni / Genazzani, Armando A. et al. | 2006
- 471
-
Identification and Biological Characterization of 6-Aryl-7-isopropylquinazolinones as Novel TRPV1 Antagonists that Are Effective in Models of Chronic PainCulshaw, Andrew J. / Bevan, Stuart / Christiansen, Martin / Copp, Prafula / Davis, Andrew / Davis, Clare / Dyson, Alex / Dziadulewicz, Edward K. / Edwards, Lee / Eggelte, Hendrikus et al. | 2006
- 475
-
Insight into the Structural Requirements of Urokinase-Type Plasminogen Activator Inhibitors Based on 3D QSAR CoMFA/CoMSIA ModelsBhongade, Bhoomendra A. / Gadad, Andanappa K. et al. | 2006
- 490
-
Knowledge-Based Design of Target-Focused Libraries Using Protein−Ligand Interaction ConstraintsDeng, Zhan / Chuaqui, Claudio / Singh, Juswinder et al. | 2006
- 501
-
Computational Study of Antagonist-a1A Adrenoceptor ComplexesObservations of Conformational Variations on the Formation of Ligand-Receptor ComplexesKinsella, G.K. et al. | 2006
- 501
-
Computational Study of Antagonist/alpha~1~A Adrenoceptor Complexes-Observations of Conformational Variations on the Formation of Ligand/Receptor ComplexesKinsella, G. K. / Rozas, I. / Watson, G. W. et al. | 2006
- 501
-
Computational Study of Antagonist/α1A Adrenoceptor ComplexesObservations of Conformational Variations on the Formation of Ligand/Receptor ComplexesKinsella, Gemma K. / Rozas, Isabel / Watson, Graeme W. et al. | 2006
- 511
-
Metal-Mediated Inhibition of Escherichia c oli Methionine Aminopeptidase: Structure−Activity Relationships and Development of a Novel Scoring Function for Metal−Ligand InteractionsSchiffmann, Rolf / Neugebauer, Alexander / Klein, Christian D. et al. | 2006
- 523
-
Classification of Chemical Compounds by Protein−Compound Docking for Use in Designing a Focused LibraryFukunishi, Yoshifumi / Mikami, Yoshiaki / Takedomi, Kei / Yamanouchi, Masaya / Shima, Hideaki / Nakamura, Haruki et al. | 2006
- 534
-
Novel Procedure for Modeling Ligand/Receptor Induced Fit EffectsSherman, Woody / Day, Tyler / Jacobson, Matthew P. / Friesner, Richard A. / Farid, Ramy et al. | 2006
- 554
-
3D-QSAR Studies on Cannabinoid CB1 Receptor Agonists: G-Protein Activation as Biological DataSalo, Outi M. H. / Savinainen, Juha R. / Parkkari, Teija / Nevalainen, Tapio / Lahtela-Kakkonen, Maija / Gynther, Jukka / Laitinen, Jarmo T. / Järvinen, Tomi / Poso, Antti et al. | 2006
- 567
-
Potent 7-Hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic Acid-Based Macrocyclic Inhibitors of Hepatitis C Virus NS3 ProteaseChen, Kevin X. / Njoroge, F. George / Pichardo, John / Prongay, Andrew / Butkiewicz, Nancy / Yao, Nanhua / Madison, Vincent / Girijavallabhan, Viyyoor et al. | 2006
- 575
-
Synthesis, Chiral Resolution, and Enantiopharmacology of a Potent 2,3-Benzodiazepine Derivative as Noncompetitive AMPA Receptor AntagonistZappalà, Maria / Postorino, Giovanna / Micale, Nicola / Caccamese, Salvatore / Parrinello, Nunziatina / Grazioso, Giovanni / Roda, Gabriella / Menniti, Frank S. / De Sarro, Giovambattista / Grasso, Silvana et al. | 2006
- 582
-
Trisubstituted Acridines as G-quadruplex Telomere Targeting Agents. Effects of Extensions of the 3,6- and 9-Side Chains on Quadruplex Binding, Telomerase Activity, and Cell ProliferationMoore, Michael J. B. / Schultes, Christoph M. / Cuesta, Javier / Cuenca, Francisco / Gunaratnam, Mekala / Tanious, Farial A. / Wilson, W. David / Neidle, Stephen et al. | 2006
- 600
-
4-(3‘α15‘β-Dihydroxy-5‘β-estran-17‘β-yl)furan-2-methyl Alcohol: An Anti-Digoxin Agent with a Novel Mechanism of ActionDeutsch, Joseph / Jang, Huang G. / Mansur, Nura / Ilovich, Ohad / Shpolansky, Uri / Galili, Dana / Feldman, Tomer / Rosen, Haim / Lichtstein, David et al. | 2006
- 600
-
4-(3'a15'b-Dihydroxy-5'b-estran-17'&bgr- ;-yl)furan-2-methyl Alcohol: An Anti-Digoxin Agent with a Novel Mechanism of ActionDeutsch, J. et al. | 2006
- 600
-
4-(3'alpha15'beta-Dihydroxy-5'beta- estran-17'beta-yl)furan-2-methyl Alcohol: An Anti-Digoxin Agent with a Novel Mechanism of ActionDeutsch, J. / Jang, H. G. / Mansur, N. / Ilovich, O. / Shpolansky, U. / Galili, D. / Feldman, T. / Rosen, H. / Lichtstein, D. et al. | 2006
- 607
-
Library Design, Synthesis, and Screening: Pyridine Dicarbonitriles as Potential Prion Disease TherapeuticsReddy, Tummala R. K. / Mutter, Roger / Heal, William / Guo, Kai / Gillet, Valerie J. / Pratt, Steven / Chen, Beining et al. | 2006
- 616
-
Identification of the Key Residue of Calcitonin Gene Related Peptide (CGRP) 27−37 to Obtain Antagonists with Picomolar Affinity at the CGRP ReceptorLang, Manja / De Pol, Silvia / Baldauf, Carsten / Hofmann, Hans-Jörg / Reiser, Oliver / Beck-Sickinger, Annette G. et al. | 2006
- 625
-
3D-QSAR Studies of Arylpyrazole Antagonists of Cannabinoid Receptor Subtypes CB1 and CB2. A Combined NMR and CoMFA ApproachChen, Jian-Zhong / Han, Xiu-Wen / Liu, Qian / Makriyannis, Alexandros / Wang, Junmei / Xie, Xiang-Qun et al. | 2006
- 637
-
Overlapping, Nonidentical Binding Sites of Different Classes of Nonpeptide Antagonists for the Human Gonadotropin-Releasing Hormone ReceptorBetz, Stephen F. / Reinhart, Greg J. / Lio, Francisco M. / Chen / Struthers, R. Scott et al. | 2006
- 648
-
Protein−Protein Interactions: Modeling the Hepatitis C Virus Ion Channel p7Patargias, George / Zitzmann, Nicole / Dwek, Raymond / Fischer, Wolfgang B. et al. | 2006
- 656
-
Discovery of a Potent Inhibitor of the Antiapoptotic Protein Bcl-xL from NMR and Parallel SynthesisPetros, Andrew M. / Dinges, Jurgen / Augeri, David J. / Baumeister, Steven A. / Betebenner, David A. / Bures, Mark G. / Elmore, Steven W. / Hajduk, Philip J. / Joseph, Mary K. / Landis, Shelley K. et al. | 2006
- 664
-
The First Potent Inhibitors for Human Glutaminyl Cyclase: Synthesis and Structure−Activity RelationshipBuchholz, Mirko / Heiser, Ulrich / Schilling, Stephan / Niestroj, André J. / Zunkel, Katrin / Demuth, Hans-Ulrich et al. | 2006
- 678
-
Discovery of Two Novel, Small-Molecule Inhibitors of DNA MethylationSiedlecki, Pawel / Boy, Regine Garcia / Musch, Tanja / Brueckner, Bodo / Suhai, Sandor / Lyko, Frank / Zielenkiewicz, Piotr et al. | 2006
- 684
-
Structure−Activity Study of Brassinin Derivatives as Indoleamine 2,3-Dioxygenase InhibitorsGaspari, Paul / Banerjee, Tinku / Malachowski, William P. / Muller, Alexander J. / Prendergast, George C. / DuHadaway, James / Bennett, Shauna / Donovan, Ashley M. et al. | 2006
- 693
-
Miliusanes, A Class of Cytotoxic Agents from Miliusa sinensisZhang, Hong-Jie / Ma, Cuiying / Hung, Nguyen Van / Cuong, Nguyen Manh / Tan, Ghee Teng / Santarsiero, Bernard D. / Mesecar, Andrew D. / Soejarto, D. Doel / Pezzuto, John M. / Fong, Harry H. S. et al. | 2006
- 709
-
Synthesis and Biological Activity of Isoxazolidinyl Polycyclic Aromatic Hydrocarbons: Potential DNA IntercalatorsRescifina, Antonio / Chiacchio, Maria A. / Corsaro, Antonino / De Clercq, Erik / Iannazzo, Daniela / Mastino, Antonio / Piperno, Anna / Romeo, Giovanni / Romeo, Roberto / Valveri, Vincenza et al. | 2006
- 716
-
(+)-(2R,5S)-4-[4-Cyano-3-(trifluoromethyl)phenyl]-2,5-d- imethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an Orally Potent and Peripherally Selective Nonsteroidal Androgen Receptor Antagonist1Kinoyama, I. et al. | 2006
- 716
-
(+)-(2R,5S)-4-[4-Cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an Orally Potent and Peripherally Selective Nonsteroidal Androgen Receptor AntagonistKinoyama, Isao / Taniguchi, Nobuaki / Toyoshima, Akira / Nozawa, Eisuke / Kamikubo, Takashi / Imamura, Masakazu / Matsuhisa, Akira / Samizu, Kiyohiro / Kawanimani, Eiji / Niimi, Tatsuya et al. | 2006
- 727
-
Structure−Activity Relationship Studies of Novel Benzophenones Leading to the Discovery of a Potent, Next Generation HIV Nonnucleoside Reverse Transcriptase InhibitorRomines, Karen R. / Freeman, George A. / Schaller, Lee T. / Cowan, Jill R. / Gonzales, Steve S. / Tidwell, Jeffrey H. / Andrews, Clarence W. / Stammers, David K. / Hazen, Richard J. / Ferris, Robert G. et al. | 2006
- 740
-
Wortmannin-C20 Conjugates Generate WortmanninYuan, Hushan / Luo, Ji / Weissleder, Ralph / Cantley, Lewis / Josephson, Lee et al. | 2006
- 748
-
Novel 5α-Reductase Inhibitors: Synthesis, Structure−Activity Studies, and Pharmacokinetic Profile of Phenoxybenzoylphenyl Acetic AcidsSalem, Ola I. A. / Frotscher, Martin / Scherer, Christiane / Neugebauer, Alexander / Biemel, Klaus / Streiber, Martina / Maas, Ruth / Hartmann, Rolf W. et al. | 2006
- 748
-
Novel 5alpha-Reductase Inhibitors: Synthesis, Structure-Activity Studies, and Pharmacokinetic Profile of Phenoxybenzoylphenyl Acetic AcidsSalem, O. I. A. / Frotscher, M. / Scherer, C. / Neugebauer, A. / Biemel, K. / Streiber, M. / Maas, R. / Hartmann, R. W. et al. | 2006
- 748
-
Novel 5a-Reductase Inhibitors: Synthesis, Structure-Activity Studies, and Pharmacokinetic Profile of Phenoxybenzoylphenyl Acetic AcidsSalem, O.I.A. et al. | 2006
- 760
-
Dopamine-Serotonin Receptor Ligands. 10:1 SAR Studies on Azecine-type Dopamine Receptor Ligands by Functional Screening at Human Cloned D1, D2L, and D5 Receptors with a Microplate Reader Based Calcium Assay Lead to a Novel Potent D1-D5 Selective AntagonistHoefgen, B. et al. | 2006
- 760
-
Dopamine/Serotonin Receptor Ligands. 10: SAR Studies on Azecine-type Dopamine Receptor Ligands by Functional Screening at Human Cloned D1, D2L, and D5 Receptors with a Microplate Reader Based Calcium Assay Lead to a Novel Potent D1/D5 Selective AntagonistHoefgen, Barbara / Decker, Michael / Mohr, Patrick / Schramm, Astrid M. / Rostom, Sherif A. F. / El-Subbagh, Hussein / Schweikert, Peter M. / Rudolf, Dirk R. / Kassack, Matthias U. / Lehmann, Jochen et al. | 2006
- 770
-
Prodrug Forms of N-[(4-Deoxy-4-amino-10-methyl)-pteroyl]glutamate-gamma-[psiP(O)(OH)]-glutarate, a Potent Inhibitor of Folylpoly-gamma-glutamate Synthetase: Synthesis and Hydrolytic StabilityFeng, Y. / Coward, J. K. et al. | 2006
- 770
-
Prodrug Forms of N-[(4-Deoxy-4-amino-10-methyl)pteroyl]glutamate-γ-[ψP(O)(OH)]-glutarate, a Potent Inhibitor of Folylpoly-γ-glutamate Synthetase: Synthesis and Hydrolytic StabilityFeng, Yan / Coward, James K. et al. | 2006
- 789
-
Synthesis and Biological Evaluation of Novel Phenylcarbazoles as Potential Anticancer AgentsRoutier, Sylvain / Mérour, Jean-Yves / Dias, Nathalie / Lansiaux, Amélie / Bailly, Christian / Lozach, Olivier / Meijer, Laurent et al. | 2006
- 800
-
Aromatic Sulfide Inhibitors of Histone Deacetylase Based on Arylsulfiny1-2,4-hexadienoic Acid HydroxyamidesMarson, C. M. / Savy, P. / Rioja, A. S. / Mahadevan, T. / Mikol, C. / Veerupillai, A. / Nsubuga, E. / Chahwan, A. / Joel, S. P. et al. | 2006
- 800
-
Aromatic Sulfide Inhibitors of Histone Deacetylase Based on Arylsulfinyl-2,4-hexadienoic Acid HydroxyamidesMarson, Charles M. / Savy, Pascal / Rioja, Alphonso S. / Mahadevan, Thevaki / Mikol, Catherine / Veerupillai, Arthi / Nsubuga, Eva / Chahwan, Angela / Joel, Simon P. et al. | 2006
- 806
-
Synthesis and in Vitro Antileukemic Activity of Some New 1,3-(Oxytetraethylenoxy)cyclotriphosphazene Derivatives §Siwy, Mariola / Sȩk, Danuta / Kaczmarczyk, Bożena / Jaroszewicz, Iwona / Nasulewicz, Anna / Pelczyñska, Marzena / Nevozhay, Dmitry / Opolski, Adam et al. | 2006
- 811
-
Correlation of Antifungal Activity with Fungal Phospholipase Inhibition Using a Series of Bisquaternary Ammonium SaltsNg, Clarissa K. L. / Obando, Daniel / Widmer, Fred / Wright, Lesley C. / Sorrell, Tania C. / Jolliffe, Katrina A. et al. | 2006
- 817
-
Orally Active Purine-Based Inhibitors of the Heat Shock Protein 90Biamonte, Marco A. / Shi, Jiandong / Hong, Kevin / Hurst, David C. / Zhang, Lin / Fan, Junhua / Busch, David J. / Karjian, Patricia L. / Maldonado, Angelica A. / Sensintaffar, John L. et al. | 2006
- 829
-
Synthesis and in Vitro Antitumor Activity of Platinum Acetonimine ComplexesBoccarelli, Angelina / Intini, Francesco P. / Sasanelli, Rossella / Sivo, Maria F. / Coluccia, Mauro / Natile, Giovanni et al. | 2006
- 838
-
Frontiers in Drug Design and Discovery. Volume 1. Edited by Gary W. Caldwell, Atta-ur-Rahman, and Barry A. Springer. Bentham Science Publishers Ltd., Hilversum, The Netherlands. 2005. vi + 360 pp. 18 × 25 cm. ISBN 90-77527-03-06. $130.00.Wolff, Manfred E. et al. | 2006
- 838
-
Named Organic Reactions. Second Edition By Thomas Laue and Andreas Plagens. Wiley & Sons, Ltd., Chichester, England. 2005. x + 310 pp. 15 × 23 cm. ISBN 0-470-01041. $55.00.Griffith, Robert K. et al. | 2006
- 838
-
Frontiers in Drug Design and Discovery. Volume 1Wolff, M. E. et al. | 2006
- 838
-
Named Organic Reactions. Second Edition. By Thomas Laue and Andreas PlagensGriffith, R. K. et al. | 2006