Journal of Medicinal Chemistry
Volume 43, Issue 3 (February 10, 2000)
Copyright © 2000 American Chemical Society

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PERSPECTIVES

305-341

Protease Inhibitors: Current Status and Future Prospects Donmienne Leung, Giovanni Abbenante, and David P. Fairlie [Full Article - PDF]

COMMUNICATIONS

342-345

A Novel, Potent, and Selective 5-HT7 Antagonist: (R)-3-(2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl)phenol (SB-269970) Peter J. Lovell, Steven M. Bromidge, Steven Dabbs, D. Malcolm Duckworth, Ian T. Forbes, Andrew J. Jennings, Frank D. King, Derek N. Middlemiss, Shirley K. Rahman, Damian V. Saunders, Lissa L. Collin, Jim J. Hagan, Graham J. Riley, and David R. Thomas [Full Article - PDF]

346-350

-Substituted N-(Sulfonamido)alkyl--aminotetralins: Potent and Selective Neuropeptide Y Y5 Receptor Antagonists Mark A. Youngman, James J. McNally, Timothy W. Lovenberg, Allen B. Reitz, Nicole M. Willard, Diane H. Nepomuceno, Sandy J. Wilson, Jeffrey J. Crooke, Daniel Rosenthal, Anil H. Vaidya, and Scott L. Dax [Full Article - PDF]

EXPEDITED ARTICLES

351-360

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 Studies Shaomeng Wang, Sukumar Sakamuri, Istvan J. Enyedy, Alan P. Kozikowski, Olivier Deschaux, Bidhan C. Bandyopadhyay, Srihari R. Tella, Wahiduz A. Zaman, and Kenneth M. Johnson [Full Article - PDF]

ARTICLES

361-368

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 P1 Lakshmi S. Narasimhan, J. Ronald Rubin, Debra R. Holland, Janet S. Plummer, Stephen T. Rapundalo, Jeremy E. Edmunds, Yves St-Denis, M. Arshad Siddiqui, and Christine Humblet [Full Article - PDF]

369-380

Design and Synthesis of Piperazine-Based Matrix Metalloproteinase Inhibitors Menyan Cheng, Biswanath De, Stanislaw Pikul, Neil G. Almstead, Michael G. Natchus, Melanie V. Anastasio, Sara J. McPhail, Catherine E. Snider, Yetunde O. Taiwo, Longyin Chen, C. Michelle Dunaway, Fei Gu, Martin E. Dowty, Glen E. Mieling, Michael J. Janusz, and Sherry Wang-Weigand [Full Article - PDF]

381-391

Molecular Docking Reveals a Novel Binding Site Model for Fentanyl at the -Opioid Receptor Govindan Subramanian, M. Germana Paterlini, Philip S. Portoghese, and David M. Ferguson [Full Article - PDF]

392-400

Derivation of Pharmacophore and CoMFA Models for Leukotriene D4 Receptor Antagonists of the Quinolinyl(bridged)aryl Series Albert Palomer, Jaume Pascual, Francesc Cabré, M. Lluïsa García, and David Mauleón [Full Article - PDF]

401-408

Successful Virtual Screening of a Chemical Database for Farnesyltransferase Inhibitor Leads Emanuele Perola, Kun Xu, Thomas M. Kollmeyer, Scott H. Kaufmann, Franklyn G. Prendergast, and Yuan-Ping Pang [Full Article - PDF]

409-419

Syntheses and Structure-Activity Relationships of 5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline Derivatives with Retinoic Acid Receptor Agonistic Activity Kouichi Kikuchi, Shigeki Hibi, Hiroyuki Yoshimura, Naoki Tokuhara, Kenji Tai, Takayuki Hida, Toshihiko Yamauchi, and Mitsuo Nagai [Full Article - PDF]

420-431

Synthesis, Molecular Modeling, and Pharmacological Testing of Bis-Quinolinium Cyclophanes: Potent, Non-Peptidic Blockers of the Apamin-Sensitive Ca2+-Activated K+ Channel Joaquin Campos Rosa, Dimitrios Galanakis, Alessandro Piergentili, Kalpana Bhandari, C. Robin Ganellin, Philip M. Dunn, and Donald H. Jenkinson [Full Article - PDF]

432-439

Synthesis and in Vitro and in Vivo Functional Studies of Ortho-Substituted Phenylpiperazine and N-Substituted 4-N-(o-Methoxyphenyl)aminopiperidine Analogues of WAY100635 Marguérite M. Mensonides-Harsema, Yi Liao, Henning Böttcher, Gerd D. Bartoszyk, Hartmunt E. Greiner, Jürgen Harting, Peter de Boer, and Håkan V. Wikström [Full Article - PDF]

440-448

Water-Soluble Phosphate Prodrugs of 1-Propargyl-8-styrylxanthine Derivatives, A2A-Selective Adenosine Receptor Antagonists Roland Sauer, Juris Maurinsh, Ulrike Reith, Friederike Fülle, Karl-Norbert Klotz, and Christa E. Müller [Full Article - PDF]

449-456

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 Antagonist Liqi He, Paul J. Gilligan, Robert Zaczek, Lawrence W. Fitzgerald, John McElroy, H-S. L. Shen, Jo Anne Saye, Ned H. Kalin, Steven Shelton, David Christ, George Trainor, and Paul Hartig [Full Article - PDF]

457-466

Design of Cancer-Specific Antitumor Agents Based on Aziridinylcyclopent[b]indoloquinones Chengguo Xing, Ping Wu, and Edward B. Skibo , Robert T. Dorr [Full Article - PDF]

467-474

Acid-Catalyzed Degradation of Clarithromycin and Erythromycin B: A Comparative Study Using NMR Spectroscopy Mohd N. Mordi, Michelle D. Pelta, Valerie Boote, Gareth A. Morris, and Jill Barber [Full Article - PDF]

475-487

Drug Delivery Systems Based on Trimethyl Lock Lactonization: Poly(ethylene glycol) Prodrugs of Amino-Containing Compounds Richard B. Greenwald, Yun H. Choe, Charles D. Conover, Kwok Shum, Dechun Wu, and Maksim Royzen [Full Article - PDF]

488-504

Potent and Selective Non-Peptidic Inhibitors of Endothelin-Converting Enzyme-1 with Sustained Duration of Action Stéphane De Lombaert, Louis Blanchard, Lisa B. Stamford, Jenny Tan, Eli M. Wallace, Yoshitaka Satoh, John Fitt, Denton Hoyer, David Simonsbergen, John Moliterni, Nicholas Marcopoulos, Paula Savage, Mary Chou, Angelo J. Trapani, and Arco Y. Jeng [Full Article - PDF]

505-516

Antimalarial Activity of Compounds Interfering with Plasmodium falciparum Phospholipid Metabolism: Comparison between Mono- and Bisquaternary Ammonium Salts Michèle Calas, Marie L. Ancelin, Gérard Cordina, Philippe Portefaix, Gilles Piquet, Valérie Vidal-Sailhan, and Henri Vial [Full Article - PDF]

BRIEF ARTICLES

517-525

New Selective and Potent 5-HT1B/1D Antagonists: Chemistry and Pharmacological Evaluation of N-Piperazinylphenyl Biphenylcarboxamides and Biphenylsulfonamides Yi Liao, Henning Böttcher, Jürgen Harting, Hartmut Greiner, Christoph van Amsterdam, Thomas Cremers, Staffan Sundell, Joachim März, Wilfried Rautenberg, and Håkan Wikström [Full Article - PDF]

BOOK REVIEWS

526-526

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. Vance Novack [Full Article - PDF]