COMMUNICATIONS
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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
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ARTICLES
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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
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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
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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
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5095-5099
Properties of Known Drugs. 2. Side Chains
Guy W. Bemis and
Mark A. Murcko
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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
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5110-5119
Predicting Relative Binding Free Energies of Tacrine-Huperzine A Hybrids as Inhibitors of Acetylcholinesterase
Xavier Barril,
Modesto Orozco, and
F. Javier Luque
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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
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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
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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
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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 -
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5160-5168
Quantitative Structure-Metabolism Relationships: Steric and Nonsteric Effects in the Enzymatic Hydrolysis of Noncongener Carboxylic Esters
Peter Buchwald and
Nicholas Bodor
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5169-5180
Simple Linear QSAR Models Based on Quantum Similarity Measures
Lluís Amat and
Ramon Carbó-Dorca
, Robert Ponec
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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]
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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]
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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]
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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]
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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]
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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]
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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]
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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]
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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]
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BRIEF ARTICLES
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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]
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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]
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BOOK REVIEWS
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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
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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
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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
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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
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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
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ADDITIONS AND CORRECTIONS
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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] | |