Journal of Medicinal Chemistry
Volume 42, Issue 25 (December 16, 1999)
Copyright © 1999 American Chemical Society

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COMMUNICATIONS

5061-5063

Discovery of the First Potent and Selective Small Molecule Opioid Receptor-like (ORL1) Antagonist: 1-[(3R,4R)-1-Cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl- 1,3-dihydro-2H-benzimidazol-2-one (J-113397) Hiroshi Kawamoto, Satoshi Ozaki, Yoshiki Itoh, Mitsuru Miyaji, Sachie Arai, Hiroshi Nakashima, Tetsuya Kato, Hisashi Ohta, and Yoshikazu Iwasawa [Full Article - PDF]

ARTICLES

5064-5071

2 Adrenoceptor Agonists as Potential Analgesic Agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles Robert E. Boyd, Jeffery B. Press, C. Royce Rasmussen, Robert B. Raffa, Ellen E. Codd, Charlene D. Connelly, Debra J. Bennett, Alex L. Kirifides, Joseph F. Gardocki, Brian Reynolds, John T. Hortenstein, and Allen B. Reitz [Full Article - PDF]

5072-5076

Combining in Vitro and in Vivo Pharmacokinetic Data for Prediction of Hepatic Drug Clearance in Humans by Artificial Neural Networks and Multivariate Statistical Techniques Gisbert Schneider, Philippe Coassolo, and Thierry Lavé [Full Article - PDF]

5077-5094

Synthesis and SAR of Adatanserin: Novel Adamantyl Aryl- and Heteroarylpiperazines with Dual Serotonin 5-HT1A and 5-HT2 Activity as Potential Anxiolytic and Antidepressant Agents Magid A. Abou-Gharbia, Wayne E. Childers, Jr., Horace Fletcher, Georgia McGaughey, Usha Patel, Michael B. Webb, John Yardley, Terrance Andree, Carl Boast, Robert J. Kucharik, Jr., Karen Marquis, Herman Morris, Rosemary Scerni, and John A. Moyer [Full Article - PDF]

5095-5099

Properties of Known Drugs. 2. Side Chains Guy W. Bemis and Mark A. Murcko [Full Article - PDF]

5100-5109

Consensus Scoring: A Method for Obtaining Improved Hit Rates from Docking Databases of Three-Dimensional Structures into Proteins Paul S. Charifson, Joseph J. Corkery, Mark A. Murcko, and W. Patrick Walters [Full Article - PDF]

5110-5119

Predicting Relative Binding Free Energies of Tacrine-Huperzine A Hybrids as Inhibitors of Acetylcholinesterase Xavier Barril, Modesto Orozco, and F. Javier Luque [Full Article - PDF]

5120-5130

Design, Synthesis, and Evaluations of Substituted 3-[(3- or 4-Carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as Inhibitors of VEGF, FGF, and PDGF Receptor Tyrosine Kinases Li Sun, Ngoc Tran, Congxin Liang, Flora Tang, Audie Rice, Randall Schreck, Kara Waltz, Laura K. Shawver, Gerald McMahon, and Cho Tang [Full Article - PDF]

5131-5141

Synthesis, in Vitro Antiproliferative Activity, and DNA-Binding Properties of Hybrid Molecules Containing Pyrrolo[2,1-c][1,4]benzodiazepine and Minor-Groove-Binding Oligopyrrole Carriers Pier Giovanni Baraldi, Gianfranco Balboni, Barbara Cacciari, Andrea Guiotto, Stefano Manfredini, Romeo Romagnoli, Giampiero Spalluto, David E. Thurston, Philip W. Howard, Nicoletta Bianchi, Cristina Rutigliano, Carlo Mischiati, and Roberto Gambari [Full Article - PDF]

5142-5152

Binding Constants of Neuraminidase Inhibitors: An Investigation of the Linear Interaction Energy Method Ian D. Wall, Andrew R. Leach, David W. Salt, Martyn G. Ford, and Jonathan W. Essex [Full Article - PDF]

5153-5159

Abasic Site Recognition in DNA as a New Strategy To Potentiate the Action of Anticancer Alkylating Drugs? Philippe Belmont, Muriel Jourdan, Martine Demeunynck, Jean-François Constant, Julian Garcia, and Jean Lhomme , Danièle Carez and Alain Croisy [Full Article - PDF]

5160-5168

Quantitative Structure-Metabolism Relationships: Steric and Nonsteric Effects in the Enzymatic Hydrolysis of Noncongener Carboxylic Esters Peter Buchwald and Nicholas Bodor [Full Article - PDF]

5169-5180

Simple Linear QSAR Models Based on Quantum Similarity Measures Lluís Amat and Ramon Carbó-Dorca , Robert Ponec [Full Article - PDF]

5181-5187

A Series of 6- and 7-Piperazinyl- and -Piperidinylmethylbenzoxazinones with Dopamine D4 Antagonist Activity: Discovery of a Potential Atypical Antipsychotic Agent Thomas R. Belliotti, David J. Wustrow, Wouter A. Brink, Kim T. Zoski, Yu-Hsin Shih, Steven Z. Whetzel, Lynn M. Georgic, Ann E. Corbin, Hyacinth C. Akunne, Thomas G. Heffner, Thomas A. Pugsley, and Lawrence D. Wise [Full Article - PDF]

5188-5196

Potential Multifunctional Inhibitors of HIV-1 Reverse Transcriptase. Novel [AZT]-[TSAO-T] and [d4T]-[TSAO-T] Heterodimers Modified in the Linker and in the Dideoxynucleoside Region Sonsoles Velázquez, Victoria Tuñón, María Luisa Jimeno, Cristina Chamorro, Erik De Clercq, Jan Balzarini, and María José Camarasa [Full Article - PDF]

5197-5211

Investigation of Subsite Preferences in Aminopeptidase A (EC 3.4.11.7) Led to the Design of the First Highly Potent and Selective Inhibitors of This Enzyme Christelle David, Laurent Bischoff, Hervé Meudal, Aurélie Mothé, Nadia De Mota, Sophie DaNascimento, Catherine Llorens-Cortes, Marie-Claude Fournié-Zaluski, and Bernard P. Roques [Full Article - PDF]

5212-5223

Design, Synthesis, and Biological Evaluation of Symmetrically and Unsymmetrically Substituted Methoctramine-Related Polyamines as Muscular Nicotinic Receptor Noncompetitive Antagonists Michela Rosini, Roberta Budriesi, M. Gabriele Bixel, Maria L. Bolognesi, Alberto Chiarini, Ferdinand Hucho, Povl Krogsgaard-Larsen, Ian R. Mellor, Anna Minarini, Vincenzo Tumiatti, Peter N. R. Usherwood, and Carlo Melchiorre [Full Article - PDF]

5224-5234

Analogues of Neuroactive Polyamine Wasp Toxins That Lack Inner Basic Sites Exhibit Enhanced Antagonism Toward a Muscle-Type Mammalian Nicotinic Acetylcholine Receptor Kristian Strmgaard, Matthew J. Brierley, Kim Andersen, Frank A. Slk, Ian R. Mellor, Peter N. R. Usherwood, Povl Krogsgaard-Larsen, and Jerzy W. Jaroszewski [Full Article - PDF]

5235-5240

New Quaternary Ammonium Oxicam Derivatives Targeted toward Cartilage: Synthesis, Pharmacokinetic Studies, and Antiinflammatory Potency Colette Nicolas, Michel Verny, Isabelle Giraud, Monique Ollier, Maryse Rapp, Jean-Claude Maurizis, and Jean-Claude Madelmont [Full Article - PDF]

5241-5253

Discovery and Structure-Activity Relationships of Imidazole-Containing Tetrahydrobenzodiazepine Inhibitors of Farnesyltransferase Charles Z. Ding, Roberta Batorsky, Rajeev Bhide, Hannguang J. Chao, Young Cho, Saeho Chong, Johnni Gullo-Brown, Peng Guo, Soong Hoon Kim, Frank Lee, Katerina Leftheris, Arthur Miller, Toomas Mitt, Manorama Patel, Becky A. Penhallow, Carol Ricca, William C. Rose, Robert Schmidt, William A. Slusarchyk, Gregory Vite, Ning Yan, Veeraswamy Manne, and John T. Hunt [Full Article - PDF]

5254-5265

Potent, Orally Active GPIIb/IIIa Antagonists Containing a Nipecotic Acid Subunit. Structure-Activity Studies Leading to the Discovery of RWJ-53308 William J. Hoekstra, Bruce E. Maryanoff, Bruce P. Damiano, Patricia Andrade-Gordon, Judith H. Cohen, Michael J. Costanzo, Barbara J. Haertlein, Leonard R. Hecker, Becky L. Hulshizer, Jack A. Kauffman, Patricia Keane, David F. McComsey, John A. Mitchell, Lorraine Scott, Rekha D. Shah, and Stephen C. Yabut [Full Article - PDF]

5266-5271

Vasorelaxation by New Hybrid Compounds Containing Dihydropyridine and Pinacidil-Like Moieties Lev M. Yagupolskii, Wolfram Antepohl, Ferruh Artunc, Renate Handrock, Boris M. Klebanov, Irina I. Maletina, Bent Marxen, Kirill I. Petko, Ulrich Quast, Anna Vogt, Carolin Weiss, Jutta Zibold, and Stefan Herzig [Full Article - PDF]

BRIEF ARTICLES

5272-5276

N-Deacetyl-N-aminoacylthiocolchicine Derivatives: Synthesis and Biological Evaluation on MDR-Positive and MDR-Negative Human Cancer Cell Lines Maria Luisa Gelmi, Sabrina Mottadelli, and Donato Pocar , Antonella Riva and Ezio Bombardelli , Rosa De Vincenzo and Giovanni Scambia [Full Article - PDF]

5277-5283

Synthesis and Biological Evaluation of Novel Prodrugs of Anthracyclines for Selective Activation by the Tumor-Associated Protease Plasmin Franciscus M. H. de Groot, Anton C. W. de Bart, Jan H. Verheijen, and Hans W. Scheeren [Full Article - PDF]

BOOK REVIEWS

5284-5284

Rational Drug Design Edited by D. G. Truhlar, W. J. Howe, A. J. Hopfinger, J. Blaney, and R. Dammkoehler. Springer-Verlag, New York. 1999. xxii + 206 pp. 16 × 24 cm. ISBN 0-387-98753-3. $69.95. Donald J. Abraham [Full Article - PDF]

5284-5285

Second Supplements to the Second Edition of Rodd's Chemistry of Carbon Compounds. Volume IV: Heterocyclic Compounds. Part G. Six-membered Heterocyclic Compounds with (a) a Single Nitrogen Atom in the Ring (cont'd.); Polycyclic Fused Ring Compounds, (b) an Atom of Phosphorus, Arsenic, Antimony or Bismuth. Alkaloids with a Six-Membered Heterocyclic Ring (Chapters 34-35 in this volume). Part H: Six-membered Fused-Ring Heterocyclic Compounds with a Single Atom in the Ring (cont'd.). Monocyclic Ring Compounds with Two Hetero-Atoms in the Ring from Group VIB, or One Each from Groups V and VIB. Alkaloids (cont'd.) Edited by M. Sainsbury. Elsevier, Amsterdam, 1998. xx + 650 pp. 15.5 × 23 cm. ISBN 0-444-82979-2. $402.50. Arnold Martin [Full Article - PDF]

5285-5285

Protective Groups in Organic Synthesis. Third Edition By Theodora W. Greene and Peter G. M. Wuts. John Wiley & Sons, New York. 1999. xxi + 779 pp. 16 × 24 cm. ISBN 0-471-16019-9. $84.95. Mitchell A. Avery [Full Article - PDF]

5285-5286

Stereoselectivity in Synthesis By Tse-Lok Ho. John Wiley & Sons, New York. 1999. xv + 333 pp. 16 × 24.5 cm. ISBN 0471329223. $94.95. Patrick Dussault [Full Article - PDF]

5286-5287

Topics in Stereochemistry, Volume 22 Edited by Scott E. Denmark. Wiley Interscience, New York. 1999. xii + 314 pp. 16 × 23.5 cm. ISBN 0-471-25316-2. $95.00. G. Marc Loudon [Full Article - PDF]

ADDITIONS AND CORRECTIONS

5288-5288

Synthesis, Pharmacological and Biophysical Characterization, and Membrane-Interaction QSAR Analysis of Cationic Amphiphilic Model Compounds. Christian D. P. Klein, Martin Christiane Schellinski, Silke Landmann, Stefanie Hauschild, Dieter Heber, Klaus Mohr, and A. J. Hopfinger: [Full Article - PDF]

5288-5288

Discovery and Structure-Activity Relationships of Imidazole-Containing Tetrahydrobenzodiazepine Inhibitors of Farnesyltransferase. Charles Z. Ding, Roberta Batorsky, Rajeev Bhide, Hannguang J. Chao, Young Cho, Saeho Chong, Johnni Gullo-Brown, Peng Guo, Soong Hoon Kim, Frank Lee, Katerina Leftheris, Arthur Miller, Toomas Mitt, Manorama Patel, Becky A. Penhallow, Carol Ricca, William C. Rose, Robert Schmidt, William A. Slusarchyk, Gregory Vite, Ning Yan, Veeraswamy Manne, and John T. Hunt: [Full Article - PDF]