Naphthyl and Coumarinyl Biarylpiperazine Derivatives as Highly Potent Human beta-Secretase Inhibitors. Design, Synthesis, and Enzymatic BACE-1 and Cell Assays (English)
- New search for: Garino, C.
- New search for: Tomita, T.
- New search for: Pietrancosta, N.
- New search for: Laras, Y.
- New search for: Rosas, R.
- New search for: Herbette, G.
- New search for: Maigret, B.
- New search for: Quelever, G.
- New search for: Iwatsubo, T.
- New search for: Kraus, J.-L.
- New search for: Garino, C.
- New search for: Tomita, T.
- New search for: Pietrancosta, N.
- New search for: Laras, Y.
- New search for: Rosas, R.
- New search for: Herbette, G.
- New search for: Maigret, B.
- New search for: Quelever, G.
- New search for: Iwatsubo, T.
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In:
JOURNAL OF MEDICINAL CHEMISTRY
;
49
, 14
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4275-4285
;
2006
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ISSN:
- Article (Journal) / Print
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Title:Naphthyl and Coumarinyl Biarylpiperazine Derivatives as Highly Potent Human beta-Secretase Inhibitors. Design, Synthesis, and Enzymatic BACE-1 and Cell Assays
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Contributors:Garino, C. ( author ) / Tomita, T. ( author ) / Pietrancosta, N. ( author ) / Laras, Y. ( author ) / Rosas, R. ( author ) / Herbette, G. ( author ) / Maigret, B. ( author ) / Quelever, G. ( author ) / Iwatsubo, T. ( author ) / Kraus, J.-L. ( author )
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Published in:JOURNAL OF MEDICINAL CHEMISTRY ; 49, 14 ; 4275-4285
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Publisher:
- New search for: ACS AMERICAN CHEMICAL SOCIETY
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Publication date:2006-01-01
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Size:11 pages
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ISSN:
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Type of media:Article (Journal)
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Type of material:Print
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Language:English
- New search for: 615
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Classification:
DDC: 615 -
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© Metadata Copyright the British Library Board and other contributors. All rights reserved.
Table of contents – Volume 49, Issue 14
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
- 3999
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Approaches to Antiobesity Therapy. An IntroductionBishop, Michael J. et al. | 2006
- 4001
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Obesity: The DiseaseBray, George A. et al. | 2006
- 4008
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CB1 Cannabinoid Receptor Antagonists for Treatment of Obesity and Prevention of Comorbid Metabolic DisordersAntel, Jochen / Gregory, Peter C. / Nordheim, Ulrich et al. | 2006
- 4017
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Melanin-Concentrating Hormone-1 Receptor Antagonists for the Treatment of ObesityHandlon, Anthony L. / Zhou, Huiqiang et al. | 2006
- 4023
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5-Hydroxytryptamine 2C (5-HT2C) Receptor Agonists as Potential Antiobesity AgentsNilsson, Björn M. et al. | 2006
- 4035
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Melanocortin-4 Receptor (MC4R) Agonists for the Treatment of ObesityNargund, Ravi P. / Strack, Alison M. / Fong, Tung M. et al. | 2006
- 4044
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Discovery of Novel Triazole-Based Opioid Receptor AntagonistsZhang, Qiang / Keenan, Susan M. / Peng, Youyi / Nair, Anil C. / Yu, Seong Jae / Howells, Richard D. / Welsh, William J. et al. | 2006
- 4048
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Development of Peptidic Dopamine Transporter Inhibitors via Aromatic Modification-Mediated Conformational RestrictionDing, Jinguo / Shi, Jiahao / Cui, Dafu / Xu, Linfeng / Duan, Shuhui / Guo, Lihe / Fei, Jian et al. | 2006
- 4052
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Toward Orthopoxvirus Countermeasures: A Novel Heteromorphic Nucleoside of Unusual StructureFan, Xuesen / Zhang, Xinying / Zhou, Longhu / Keith, Kathy A. / Prichard, Mark N. / Kern, Earl R. / Torrence, Paul F. et al. | 2006
- 4055
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Discovery of Potent and Orally Available Malonyl-CoA Decarboxylase Inhibitors as Cardioprotective AgentsCheng, Jie-Fei / Huang, Yujin / Penuliar, Richard / Nishimoto, Masahiro / Liu, Larry / Arrhenius, Thomas / Yang, Guang / O'Leary, Eoin / Barbosa, Miguel / Barr, Rick et al. | 2006
- 4059
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FK506-Binding Protein Ligands: Structure-Based Design, Synthesis, and Neurotrophic/Neuroprotective Properties of Substituted 5,5-Dimethyl-2-(4-thiazolidine)carboxylatesZhao, Liqin / Huang, Wei / Liu, Hongying / Wang, Lili / Zhong, Wu / Xiao, Junhai / Hu, Yuandong / Li, Song et al. | 2006
- 4072
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Design and Synthesis of the First Generation of Dithiolane Thiazolidinedione- and Phenylacetic Acid-Based PPARγ AgonistsChittiboyina, Amar G. / Venkatraman, Meenakshi S. / Mizuno, Cassia S. / Desai, Prashant V. / Patny, Akshay / Benson, Stephen C. / Ho, Christopher I. / Kurtz, Theodore W. / Pershadsingh, Harrihar A. / Avery, Mitchell A. et al. | 2006
- 4072
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Design and Synthesis of the First Generation of Dithiolane Thiazolidinedione- and Phenylacetic Acid-Based PPARgamma AgonistsChittiboyina, A. G. / Venkatraman, M. S. / Mizuno, C. S. / Desai, P. V. / Patny, A. / Benson, S. C. / Ho, C. I. / Kurtz, T. W. / Pershadsingh, H. A. / Avery, M. A. et al. | 2006
- 4085
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Pharmacophore Based Receptor Modeling: The Case of Adenosine A3 Receptor Antagonists. An Approach to the Optimization of Protein ModelsTafi, Andrea / Bernardini, Cesare / Botta, Maurizio / Corelli, Federico / Andreini, Matteo / Martinelli, Adriano / Ortore, Gabriella / Baraldi, Pier Giovanni / Fruttarolo, Francesca / Borea, Pier Andrea et al. | 2006
- 4098
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Design, Synthesis, and Structure−Activity Relationships of Novel 2-Substituted Pyrazinoylguanidine Epithelial Sodium Channel Blockers: Drugs for Cystic Fibrosis and Chronic BronchitisHirsh, Andrew J. / Molino, Bruce F. / Zhang, Jianzhong / Astakhova, Nadezhda / Geiss, William B. / Sargent, Bruce J. / Swenson, Brian D. / Usyatinsky, Alexander / Wyle, Michael J. / Boucher, Richard C. et al. | 2006
- 4116
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Secondary Amides of Sulfonylated 3-Amidinophenylalanine. New Potent and Selective Inhibitors of Matriptase †Steinmetzer, Torsten / Schweinitz, Andrea / Stürzebecher, Anne / Dönnecke, Daniel / Uhland, Kerstin / Schuster, Oliver / Steinmetzer, Peter / Müller, Friedemann / Friedrich, Rainer / Than, Manuel E. et al. | 2006
- 4127
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New 3-Alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-Dioxide Derivatives Activate ATP-Sensitive Potassium Channels of Pancreatic Beta CellsNielsen, Flemming E. / Ebdrup, Søren / Jensen, Anette Frost / Ynddal, Lars / Bodvarsdottir, Thora B. / Stidsen, Carsten / Worsaae, Anne / Boonen, Harrie C. M. / Arkhammar, Per O. G. / Fremming, Tinna et al. | 2006
- 4140
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Design, Synthesis, and Biological Evaluation of the Combinatorial Library with a New Spirodiketopiperazine Scaffold. Discovery of Novel Potent and Selective Low-Molecular-Weight CCR5 AntagonistsHabashita, Hiromu / Kokubo, Masaya / Hamano, Shin-ichi / Hamanaka, Nobuyuki / Toda, Masaaki / Shibayama, Shiro / Tada, Hideaki / Sagawa, Kenji / Fukushima, Daikichi / Maeda, Kenji et al. | 2006
- 4153
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Is the sigma~2 Receptor a Histone Binding Protein?Colabufo, N. A. / Berardi, F. / Abate, C. / Contino, M. / Niso, M. / Perrone, R. et al. | 2006
- 4153
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Is the σ2 Receptor a Histone Binding Protein?Colabufo, Nicola Antonio / Berardi, Francesco / Abate, Carmen / Contino, Marialessandra / Niso, Mauro / Perrone, Roberto et al. | 2006
- 4159
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2,5-Diketopiperazines as Potent, Selective, and Orally Bioavailable Oxytocin Antagonists. 3. Synthesis, Pharmacokinetics, and in Vivo PotencyBorthwick, Alan D. / Davies, Dave E. / Exall, Anne M. / Hatley, Richard J. D. / Hughes, Jennifer A. / Irving, Wendy R. / Livermore, David G. / Sollis, Steve L. / Nerozzi, Fabrizio / Valko, Klara L. et al. | 2006
- 4171
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Iron Binding Dendrimers: A Novel Approach for the Treatment of HaemochromatosisZhou, Tao / Neubert, Hendrik / Liu, Ding Yong / Liu, Zu Dong / Ma, Yong Min / Kong, Xiao Le / Luo, Wei / Mark, Sykes / Hider, Robert C. et al. | 2006
- 4183
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Acyclic Nucleoside Analogues as Inhibitors of Plasmodium f alciparum dUTPaseNguyen, Corinne / Ruda, Gian Filippo / Schipani, Alessandro / Kasinathan, Ganasan / Leal, Isabel / Musso-Buendia, Alexander / Kaiser, Marcel / Brun, Reto / Ruiz-Pérez, Luis M. / Sahlberg, Britt-Louise et al. | 2006
- 4196
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Activity of and Initial Mechanistic Studies on a Novel Antileishmanial Agent Identified through in Silico Pharmacophore Development and Database SearchingDelfín, Dawn A. / Bhattacharjee, Apurba K. / Yakovich, Adam J. / Werbovetz, Karl A. et al. | 2006
- 4208
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Back Door Modulation of the Farnesoid X Receptor: Design, Synthesis, and Biological Evaluation of a Series of Side Chain Modified Chenodeoxycholic Acid DerivativesPellicciari, Roberto / Gioiello, Antimo / Costantino, Gabriele / Sadeghpour, Bahman M. / Rizzo, Giovanni / Meyer, Udo / Parks, Derek J. / Entrena-Guadix, Antonio / Fiorucci, Stefano et al. | 2006
- 4216
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Dissociated Nonsteroidal Glucocorticoid Receptor Modulators; Discovery of the Agonist Trigger in a Tetrahydronaphthalene−Benzoxazine Series †Barker, Mike / Clackers, Margaret / Copley, Royston / Demaine, Derek A. / Humphreys, Davina / Inglis, Graham G. A. / Johnston, Michael J. / Jones, Haydn T. / Haase, Michael V. / House, David et al. | 2006
- 4232
-
Virtual Screening of DNA Minor Groove BindersEvans, David A. / Neidle, Stephen et al. | 2006
- 4239
-
Further Structural Exploration of Trisubstituted Asymmetric Pyran Derivatives (2S,4R,5R)-2-Benzhydryl-5-benzylamino-tetrahydropyran-4-ol and Their Corresponding Disubstituted (3S,6S) Pyran Derivatives: A Proposed Pharmacophore Model for High-Affinity Interaction with the Dopamine, Serotonin, and Norepinephrine TransportersZhang, Shijun / Fernandez, Fernando / Hazeldine, Stuart / Deschamps, Jeffrey / Zhen, Juan / Reith, Maarten E. A. / Dutta, Aloke K. et al. | 2006
- 4248
-
From Ligand to Complexes: Inhibition of Human Immunodeficiency Virus Type 1 Integrase by b-Diketo Acid Metal ComplexesSechi, M. et al. | 2006
- 4248
-
From Ligand to Complexes: Inhibition of Human Immunodeficiency Virus Type 1 Integrase by β-Diketo Acid Metal ComplexesSechi, Mario / Bacchi, Alessia / Carcelli, Mauro / Compari, Carlotta / Duce, Elenia / Fisicaro, Emilia / Rogolino, Dominga / Gates, Paul / Derudas, Marco / Al-Mawsawi, Laith Q. et al. | 2006
- 4248
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From Ligand to Complexes: Inhibition of Human Immunodeficiency Virus Type 1 Integrase by beta-Diketo Acid Metal ComplexesSechi, M. / Bacchi, A. / Carcelli, M. / Compari, C. / Duce, E. / Fisicaro, E. / Rogolino, D. / Gates, P. / Derudas, M. / Al-Mawsawi, L. Q. et al. | 2006
- 4261
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Docking and Three-Dimensional Quantitative Structure−Activity Relationship (3D QSAR) Analyses of Nonsteroidal Progesterone Receptor LigandsSöderholm, Annu A. / Lehtovuori, Pekka T. / Nyrönen, Tommi H. et al. | 2006
- 4269
-
C-(4,5,6-Trimethoxyindan-1-yl)methanamine: A Mescaline Analogue Designed Using a Homology Model of the 5-HT2A ReceptorMcLean, Thomas H. / Chambers, James J. / Parrish, Jason C. / Braden, Michael R. / Marona-Lewicka, Danuta / Kurrasch-Orbaugh, Deborah / Nichols, David E. et al. | 2006
- 4275
-
Naphthyl and Coumarinyl Biarylpiperazine Derivatives as Highly Potent Human β-Secretase Inhibitors. Design, Synthesis, and Enzymatic BACE-1 and Cell AssaysGarino, Cédrik / Tomita, Taisuke / Pietrancosta, Nicolas / Laras, Younes / Rosas, Roselyne / Herbette, Gaëtan / Maigret, Bernard / Quéléver, Gilles / Iwatsubo, Takeshi / Kraus, Jean-Louis et al. | 2006
- 4275
-
Naphthyl and Coumarinyl Biarylpiperazine Derivatives as Highly Potent Human b-Secretase Inhibitors. Design, Synthesis, and Enzymatic BACE-1 and Cell AssaysGarino, C. et al. | 2006
- 4275
-
Naphthyl and Coumarinyl Biarylpiperazine Derivatives as Highly Potent Human beta-Secretase Inhibitors. Design, Synthesis, and Enzymatic BACE-1 and Cell AssaysGarino, C. / Tomita, T. / Pietrancosta, N. / Laras, Y. / Rosas, R. / Herbette, G. / Maigret, B. / Quelever, G. / Iwatsubo, T. / Kraus, J.-L. et al. | 2006
- 4286
-
Structural Requirements for the Substrates of the H+/Peptide Cotransporter PEPT2 Determined by Three-Dimensional Quantitative Structure−Activity Relationship AnalysisBiegel, Annegret / Gebauer, Sabine / Brandsch, Matthias / Neubert, Klaus / Thondorf, Iris et al. | 2006
- 4297
-
Validation of a Novel CHX-A‘ ‘ Derivative Suitable for Peptide Conjugation: Small Animal PET/CT Imaging Using Yttrium-86-CHX-A‘ ‘-OctreotideClifford, Thomas / Boswell, C. Andrew / Biddlecombe, Gráinne B. / Lewis, Jason S. / Brechbiel, Martin W. et al. | 2006
- 4305
-
Proposal of a New Binding Orientation for Non-Peptide AT1 Antagonists: Homology Modeling, Docking and Three-Dimensional Quantitative Structure−Activity Relationship AnalysisTuccinardi, Tiziano / Calderone, Vincenzo / Rapposelli, Simona / Martinelli, Adriano et al. | 2006
- 4317
-
New Furan Side Tetracyclic Allopsoralen Derivatives: Synthesis and Photobiological EvaluationDalla Via, Lisa / Mammi, Stefano / Uriarte, Eugenio / Santana, Lourdes / Lampronti, Ilaria / Gambari, Roberto / Gia, Ornella et al. | 2006
- 4327
-
Design and Synthesis of Novel 2-Amino-5-hydroxyindole Derivatives That Inhibit Human 5-LipoxygenaseLandwehr, Jens / George, Sven / Karg, Eva-Maria / Poeckel, Daniel / Steinhilber, Dieter / Troschuetz, Reinhard / Werz, Oliver et al. | 2006
- 4333
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Design, Synthesis, and Biological Evaluation of Cyclic and Acyclic Nitrobenzylphosphoramide Mustards for E. c oli Nitroreductase ActivationJiang, Yongying / Han, Jiye / Yu, Chengzhi / Vass, Simon O. / Searle, Peter F. / Browne, Patrick / Knox, Richard J. / Hu, Longqin et al. | 2006
- 4344
-
Kinetics and Mechanisms of Activation of alpha-Amino Acid Ester Prodrugs of CamptothecinsSong, L. / Bevins, R. / Anderson, B. D. et al. | 2006
- 4344
-
Kinetics and Mechanisms of Activation of a-Amino Acid Ester Prodrugs of CamptothecinsSong, L. et al. | 2006
- 4344
-
Kinetics and Mechanisms of Activation of α-Amino Acid Ester Prodrugs of CamptothecinsSong, Lin / Bevins, Robert / Anderson, Bradley D. et al. | 2006
- 4356
-
Antitumor Activity of JS-K [O 2-(2,4-Dinitrophenyl) 1-[(4-Ethoxycarbonyl)piperazin-1-yl]diazen-1-ium-1,2-diolate] and Related O 2-Aryl Diazeniumdiolates in Vitro and in VivoShami, Paul J. / Saavedra, Joseph E. / Bonifant, Challice L. / Chu, Jingxi / Udupi, Vidya / Malaviya, Swati / Carr, Brian I. / Kar, Siddhartha / Wang, Meifeng / Jia, Lee et al. | 2006
- 4367
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Line-Walking Method for Predicting the Inhibition of P450 Drug MetabolismHudelson, Matthew G. / Jones, Jeffrey P. et al. | 2006
- 4374
-
(R)-3‘-(3-Methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5‘-oxazolidin]-2‘-one, a Novel and Potent α7 Nicotinic Acetylcholine Receptor Partial Agonist Displays Cognitive Enhancing PropertiesTatsumi, Ryo / Fujio, Masakazu / Takanashi, Shin-ichi / Numata, Atsushi / Katayama, Jiro / Satoh, Hiroyuki / Shiigi, Yasuyuki / Maeda, Jun-ichi / Kuriyama, Makoto / Horikawa, Takashi et al. | 2006
- 4374
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(R)-3'-(3-Methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo-[2,2,2]octane-3,5'-oxazolidin]-2'-one, a Novel and Potent alpha7 Nicotinic Acetylcholine Receptor Partial Agonist Displays Cognitive Enhancing PropertiesTatsumi, R. / Fujio, M. / Takanashi, S.-i. / Numata, A. / Katayama, J. / Satoh, H. / Shiigi, Y. / Maeda, J.-i. / Kuriyama, M. / Horikawa, T. et al. | 2006
- 4374
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(R)-3'-(3-Methylbenzo[b]thiophen-5-yl)spiro[1-azabi- cyclo[2,2,2]octane-3,5'-oxazolidin]-2'-one, a Novel and Potent a7 Nicotinic Acetylcholine Receptor Partial Agonist Displays Cognitive Enhancing PropertiesTatsumi, R. et al. | 2006
- 4384
-
A New Synthesis of Sulfonamides by Aminolysis of p-Nitrophenylsulfonates Yielding Potent and Selective Adenosine A2B Receptor AntagonistsYan, Luo / Bertarelli, Daniela C. G. / Hayallah, Alaa M. / Meyer, Heiko / Klotz, Karl-Norbert / Müller, Christa E. et al. | 2006
- 4392
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Semisynthetic Maytansine Analogues for the Targeted Treatment of CancerWiddison, Wayne C. / Wilhelm, Sharon D. / Cavanagh, Emily E. / Whiteman, Kathleen R. / Leece, Barbara A. / Kovtun, Yelena / Goldmacher, Victor S. / Xie, Hongsheng / Steeves, Rita M. / Lutz, Robert J. et al. | 2006
- 4409
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Novel Selective Inhibitors of Neutral Endopeptidase for the Treatment of Female Sexual Arousal Disorder. Synthesis and Activity of Functionalized GlutaramidesPryde, David C. / Maw, Graham N. / Planken, Simon / Platts, Michelle Y. / Sanderson, Vivienne / Corless, Martin / Stobie, Alan / Barber, Christopher G. / Russell, Rachel / Foster, Laura et al. | 2006
- 4425
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Discovery of N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an Agonist of the α7 Nicotinic Acetylcholine Receptor, for the Potential Treatment of Cognitive Deficits in Schizophrenia: Synthesis and Structure−Activity RelationshipWishka, Donn G. / Walker, Daniel P. / Yates, Karen M. / Reitz, Steven C. / Jia, Shaojuan / Myers, Jason K. / Olson, Kirk L. / Jacobsen, E. Jon / Wolfe, Mark L. / Groppi, Vincent E. et al. | 2006
- 4425
-
Discovery of N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c&- #93;pyridine-5-carboxamide, an Agonist of the a7 Nicotinic Acetylcholine Receptor, for the Potential Treatment of Cognitive Deficits in Schizophrenia: Synthesis and Structure-Activity RelationshipWishka, D.G. et al. | 2006
- 4425
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Discovery of N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an Agonist of the alpha7 Nicotinic Acetylcholine Receptor, for the Potential Treatment of Cognitive Deficits in Schizophrenia: Synthesis and Structure-Activity RelationshipWishka, D. G. / Walker, D. P. / Yates, K. M. / Reitz, S. C. / Jia, S. / Myers, J. K. / Olson, K. L. / Jacobsen, E. J. / Wolfe, M. L. / Groppi, V. E. et al. | 2006
- 4437
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Imidazole−Dioxolane Compounds as Isozyme-Selective Heme Oxygenase InhibitorsVlahakis, Jason Z. / Kinobe, Robert T. / Bowers, Raymond J. / Brien, James F. / Nakatsu, Kanji / Szarek, Walter A. et al. | 2006
- 4442
-
Hydroxy-1,2,5-oxadiazolyl Moiety as Bioisoster of the Carboxy Function. Synthesis, Ionization Constants, and Pharmacological Characterization of gamma-Aminobutyric Acid (GABA) Related CompoundsLolli, M. L. / Hansen, S. L. / Rolando, B. / Nielsen, B. / Wellendorph, P. / Madsen, K. / Larsen, O. M. / Kristiansen, U. / Fruttero, R. / Gasco, A. et al. | 2006
- 4442
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Hydroxy-1,2,5-oxadiazolyl Moiety as Bioisoster of the Carboxy Function. Synthesis, Ionization Constants, and Pharmacological Characterization of γ-Aminobutyric Acid (GABA) Related CompoundsLolli, Marco L. / Hansen, Suzanne L. / Rolando, Barbara / Nielsen, Birgitte / Wellendorph, Petrine / Madsen, Karsten / Larsen, Orla Miller / Kristiansen, Uffe / Fruttero, Roberta / Gasco, Alberto et al. | 2006