Journal of Medicinal Chemistry
Volume 43, Issue 9 (May 4, 2000)
Copyright © 2000 American Chemical Society

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PERSPECTIVES

1641-1660

Corticotropin Releasing Factor (CRF) Receptor Modulators: Progress and Opportunities for New Therapeutic Agents Paul J. Gilligan, David W. Robertson, and Robert Zaczek [Full Article - PDF]

COMMUNICATIONS

1661-1663

N-[[(5-Methyl-3-phenylisoxazol-4-yl)- phenyl]sulfonyl]propanamide, Sodium Salt, Parecoxib Sodium: A Potent and Selective Inhibitor of COX-2 for Parenteral Administration John J. Talley, Stephen R. Bertenshaw, David L. Brown, Jeffery S. Carter, Matthew J. Graneto, Michael S. Kellogg, Carol M. Koboldt, Jinhua Yuan, Yan Y. Zhang, and Karen Seibert [Full Article - PDF]

EXPEDITED ARTICLES

1664-1669

Potent Derivatives of Glucagon-like Peptide-1 with Pharmacokinetic Properties Suitable for Once Daily Administration Lotte B. Knudsen, Per F. Nielsen, Per O. Huusfeldt, Nils L. Johansen, Kjeld Madsen, Freddy Z. Pedersen, Henning Thgersen, Michael Wilken, and Henrik Agers [Full Article - PDF]

ARTICLES

1670-1683

Substituted Benzamide Inhibitors of Human Rhinovirus 3C Protease: Structure-Based Design, Synthesis, and Biological Evaluation Siegfried H. Reich, Theodore Johnson, Michael B. Wallace, Susan E. Kephart, Shella A. Fuhrman, Stephen T. Worland, David A. Matthews, Thomas F. Hendrickson, Fora Chan, James Meador, III, Rose Ann Ferre, Edward L. Brown, Dorothy M. DeLisle, Amy K. Patick, Susan L. Binford, and Clifford E. Ford [Full Article - PDF]

1684-1691

Molecular Determinants of MAO Selectivity in a Series of Indolylmethylamine Derivatives: Biological Activities, 3D-QSAR/CoMFA Analysis, and Computational Simulation of Ligand Recognition Jose A. Morón, Mercedes Campillo, Virgili Perez, Mercedes Unzeta, and Leonardo Pardo [Full Article - PDF]

1692-1698

Probing the Conformation of the Sugar Transport Inhibitor Phlorizin by 2D-NMR, Molecular Dynamics Studies, and Pharmacophore Analysis Susanne Wielert-Badt, Jiann-Trzuo Lin, Mike Lorenz, Stefan Fritz, and Rolf K.-H. Kinne [Full Article - PDF]

1699-1704

2-Amino-2-oxazolines as Subtype Selective 2 Adrenoceptor Agonists Wai C. Wong, Wanying Sun, Weili Cui, Yuewen Chen, Carlos Forray, Pierre J.-J. Vaysse, Theresa A. Branchek, and Charles Gluchowski [Full Article - PDF]

1705-1713

New Proline Mimetics: Synthesis of Thrombin Inhibitors Incorporating Cyclopentane- and Cyclopentenedicarboxylic Acid Templates in the P2 Position. Binding Conformation Investigated by X-ray Crystallography Daniel Nöteberg, Jonas Brånalt, Ingemar Kvarnström, Marcel Linschoten, Djordje Musil, Jan-Erik Nyström, Guido Zuccarello, and Bertil Samuelsson [Full Article - PDF]

1714-1722

Design and Synthesis of Conformationally Constrained Glucagon Analogues Dev Trivedi, Ying Lin, Jung-Mo Ahn, Mara Siegel, Nevena N. Mollova, Karl H. Schram, and Victor J. Hruby [Full Article - PDF]

1723-1740

Toward General Methods of Targeted Library Design: Topomer Shape Similarity Searching with Diverse Structures as Queries Katherine M. Andrews and Richard D. Cramer [Full Article - PDF]

1741-1753

Solution Structures in SDS Micelles and Functional Activity at the Bullfrog Substance P Receptor of Ranatachykinin Peptides Shane A. Perrine, Tracy L. Whitehead, Rickey P. Hicks, John L. Szarek, James E. Krause, and Mark A. Simmons [Full Article - PDF]

1754-1761

Characterization of the Binding Site of the Histamine H3 Receptor. 2. Synthesis, in Vitro Pharmacology, and QSAR of a Series of Monosubstituted Benzyl Analogues of Thioperamide Albert D. Windhorst, Henk Timmerman, Edward A. Worthington, Greetje J. Bijloo, Paul H. J. Nederkoorn, Wiro M. P. B. Menge, Rob Leurs, and Jacobus D. M. Herscheid [Full Article - PDF]

1762-1769

Screening of New Antioxidant Molecules Using Flow Cytometry Serge Ostrovidov, Patricia Franck, Delphine Joseph, Laurent Martarello, Gilbert Kirsch, Francine Belleville, Pierre Nabet, and Brigitte Dousset [Full Article - PDF]

1770-1779

Design of a Gag Pentapeptide Analogue that Binds Human Cyclophilin A More Efficiently than the Entire Capsid Protein: New Insights for the Development of Novel Anti-HIV-1 Drugs Quan Li, Mireille Moutiez, Jean-Baptiste Charbonnier, Karine Vaudry, André Ménez, Eric Quéméneur, and Christophe Dugave [Full Article - PDF]

1780-1792

Nuclear Receptor-DNA Binding Specificity: A COMBINE and Free-Wilson QSAR Analysis Sanja Tomic, Lennart Nilsson, and Rebecca C. Wade [Full Article - PDF]

1793-1806

Protease Inhibitors: Synthesis and QSAR Study of Novel Classes of Nonbasic Thrombin Inhibitors Incorporating Sulfonylguanidine and O-Methylsulfonylisourea Moieties at P1 Claudiu T. Supuran, Andrea Scozzafava, Fabrizio Briganti, and Brian W. Clare [Full Article - PDF]

1807-1816

Multivariate Data Analysis Using D-Optimal Designs, Partial Least Squares, and Response Surface Modeling: A Directional Approach for the Analysis of Farnesyltransferase Inhibitors Elie Giraud, Claude Luttmann, François Lavelle, Jean-François Riou, Patrick Mailliet, and Abdelazize Laoui [Full Article - PDF]

1817-1825

Synthesis and Cytostatic Activity of Substituted 6-Phenylpurine Bases and Nucleosides: Application of the Suzuki-Miyaura Cross-Coupling Reactions of 6-Chloropurine Derivatives with Phenylboronic Acids Michal Hocek, Antonín Hol, Ivan Votruba, and Hana Dvoáková [Full Article - PDF]

1826-1840

Design and Synthesis of Aryloxyethyl Thiocyanate Derivatives as Potent Inhibitors of Trypanosoma cruzi Proliferation Sergio H. Szajnman, Wen Yan, Brian N. Bailey, Roberto Docampo, Eleonora Elhalem, and Juan B. Rodriguez [Full Article - PDF]

1841-1851

1-Imidazolyl(alkyl)-Substituted Di- and Tetrahydroquinolines and Analogues: Syntheses and Evaluation of Dual Inhibitors of Thromboxane A2 Synthase and Aromatase Christoph Jacobs, Martin Frotscher, Gerd Dannhardt, and Rolf W. Hartmann [Full Article - PDF]

1852-1857

Structural Determinants of Opioid Activity in the Orvinols and Related Structures: Ethers of Orvinol and Isoorvinol Andrew Coop, Claire L. Norton, Ilona Berzetei-Gurske, Jackie Burnside, Lawrence Toll, Stephen M. Husbands, and John W. Lewis [Full Article - PDF]

1858-1865

Protease Inhibitors: Synthesis of Potent Bacterial Collagenase and Matrix Metalloproteinase Inhibitors Incorporating N-4-Nitrobenzylsulfonylglycine Hydroxamate Moieties Andrea Scozzafava and Claudiu T. Supuran [Full Article - PDF]

1866-1877

Novel Synthetic Oleanane and Ursane Triterpenoids with Various Enone Functionalities in Ring A as Inhibitors of Nitric Oxide Production in Mouse Macrophages Tadashi Honda, Gordon W. Gribble, Nanjoo Suh, Heather J. Finlay, BarbieAnn V. Rounds, Lothar Bore, Frank G. Favaloro, Jr., Yongping Wang, and Michael B. Sporn [Full Article - PDF]

1878-1885

Design and Synthesis of trans-N-[4-[2-(6-Cyano-1,2,3,4-tetrahydroisoquinolin-2- yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A Potent and Selective Dopamine D3 Receptor Antagonist with High Oral Bioavailability and CNS Penetration in the Rat Geoffrey Stemp, Tracey Ashmeade, Clive L. Branch, Michael S. Hadley, A. Jacqueline Hunter, Christopher N. Johnson, David J. Nash, Kevin M. Thewlis, Antonio K. K. Vong, Nigel E. Austin, Phillip Jeffrey, Kim Y. Avenell, Izzy Boyfield, Jim J. Hagan, Derek N. Middlemiss, Charlie Reavill, Graham J. Riley, Carole Routledge, and Martyn Wood [Full Article - PDF]

BRIEF ARTICLES

1886-1891

Structure-Based Design, Synthesis, and Biological Evaluation of Novel Pyrrolyl Aryl Sulfones: HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors Active at Nanomolar Concentrations Marino Artico, Romano Silvestri, Eugenia Pagnozzi, Biancamaria Bruno, Ettore Novellino, Giovanni Greco, Silvio Massa, Alessandro Ettorre, Anna Giulia Loi, Franca Scintu, and Paolo La Colla [Full Article - PDF]

1892-1897

Subtype-Selective N-Methyl-D-aspartate Receptor Antagonists: Benzimidazalone and Hydantoin as Phenol Replacements Robert M. Schelkun, Po-wai Yuen, Kevin Serpa, Leonard T. Meltzer, and Lawrence D. Wise , Edward R. Whittemore and Richard M. Woodward [Full Article - PDF]

BOOK REVIEWS

1898-1898

Handbook of Drug Metabolism Edited by Thomas L. Woolf. Marcel Dekker, New York. 1999. xi + 596 pp. 18 x 26 cm. ISBN 0-8247-0229-8. $225.00. D. Eric Walters [Full Article - PDF]

1898-1899

Handbook of Reagents for Organic Synthesis. Reagents, Auxiliaries, and Catalysts for C-C Bond Formation Edited by Robert M. Coates and Scott E. Denmark. John Wiley & Sons, Inc., New York. 1999. xvi + 746 pp. 22 x 28.5 cm. ISBN 0-471-97924. $115.00. Acidic and Basic Reagents. Edited by Hans J. Reich and James H. Rigby. John Wiley & Sons, Inc., New York. 1999. xii + 494 pp. 22 x 28.5 cm. ISBN 0-471-97925. $115.00. Oxidizing and Reducing Reagents. Edited by Steven D. Burke and Rick L. Danheiser. John Wiley & Sons, Inc., New York. 1999. xviii + 550 pp. 22 x 28.5 cm. ISBN 0-471-97926-0. $115.00. Activating Agents and Protecting Groups. Edited by Anthony J. Pearson and William R. Roush. John Wiley & Sons, Inc., New York. 1999. xvii + 513 pp. 22 x 28.5 cm. ISBN 0-471-97927-9. $115.00. Horacio F. Olivo [Full Article - PDF]

1899-1900

Pharmaceutical Innovation. Revolutionizing Human Health Edited by Ralph Landau, Basil Achilladelis, and Alexander Scriabine. Chemical Heritage Press, Philadelphia. 1999. xxiii + 408 pp. 16 × 24 cm. ISBN 0-941901-21-1. $44.95. Carl Kaiser [Full Article - PDF]