Table of Contents
July 18, 2002
Volume 45, Issue 15
Pages 3161-3326
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Articles
SAR Studies of Piperidine-Based Analogues of Cocaine. 4. Effect of N-Modification and Ester Replacement
Pavel A. Petukhov, Jianrong Zhang, Alan P. Kozikowski, Cheng Z. Wang, Yan Ping Ye, Kenneth M. Johnson, and Srihari R. Tella
pp 3161–3170Publication Date (Web): June 17, 2002 (Article)
DOI: 10.1021/jm0200153
Common and Selective Molecular Determinants Involved in Metabotopic Glutamate Receptor Agonist Activity
Hugues-Olivier Bertrand, Anne-Sophie Bessis, Jean-Philippe Pin, and Francine C. Acher
pp 3171–3183Publication Date (Web): June 17, 2002 (Article)
DOI: 10.1021/jm010323l
Structure Activity of 3-Aryl-1,3-diketo-Containing Compounds as HIV-1 Integrase Inhibitors1
Godwin C. G. Pais, Xuechun Zhang, Christophe Marchand, Nouri Neamati, Kiriana Cowansage, Evguenia S. Svarovskaia, Vinay K. Pathak, Yun Tang, Marc Nicklaus, Yves Pommier, and Terrence R. Burke, Jr.
pp 3184–3194Publication Date (Web): June 6, 2002 (Article)
DOI: 10.1021/jm020037p
Synthesis and Effects on Chloroquine Susceptibility in Plasmodium falciparum of a Series of New Dihydroanthracene Derivatives
Sandrine Alibert, Christiane Santelli-Rouvier, Bruno Pradines, Carole Houdoin, Daniel Parzy, Janina Karolak-Wojciechowska, and Jacques Barbe
pp 3195–3209Publication Date (Web): June 20, 2002 (Article)
DOI: 10.1021/jm011046l
4D-QSAR Analysis of a Set of Propofol Analogues: Mapping Binding Sites for an Anesthetic Phenol on the GABAA Receptor
Matthew D. Krasowski, Xuan Hong, A. J. Hopfinger, and Neil L. Harrison
pp 3210–3221Publication Date (Web): June 14, 2002 (Article)
DOI: 10.1021/jm010461a
Structure-Based Approach for Binding Site Identification on AmpC β-Lactamase
Rachel A. Powers and Brian K. Shoichet
pp 3222–3234Publication Date (Web): June 19, 2002 (Article)
DOI: 10.1021/jm020002p
Synthesis and Pharmacological Characterization of Novel Analogues of the Nicotinic Acetylcholine Receptor Agonist (±)-UB-165
Christopher G. V. Sharples, Gunter Karig, Graham L. Simpson, James A. Spencer, Emma Wright, Neil S. Millar, Susan Wonnacott, and Timothy Gallagher
pp 3235–3245Publication Date (Web): June 14, 2002 (Article)
DOI: 10.1021/jm020814l
Discovery of Aminopyridine-Based Inhibitors of Bacterial Enoyl-ACP Reductase (FabI)
William H. Miller, Mark A. Seefeld, Kenneth A. Newlander, Irene N. Uzinskas, Walter J. Burgess, Dirk A. Heerding, Catherine C. K. Yuan, Martha S. Head, David J. Payne, Stephen F. Rittenhouse, Terrance D. Moore, Stewart C. Pearson, Valerie Berry, Walter E. DeWolf, Jr., Paul M. Keller, Brian J. Polizzi, Xiayang Qiu, Cheryl A. Janson, and William F. Huffman
pp 3246–3256Publication Date (Web): June 19, 2002 (Article)
DOI: 10.1021/jm020050+
Three-Dimensional Quantitative Structure−Activity Relationship Analysis of Ligand Binding to Human Sequence Antidigoxin Monoclonal Antibodies Using Comparative Molecular Field Analysis
Carol D. Farr, Michael R. Tabet, and William J. Ball, Jr.Dianne M. FishwildXia Wang, Anil C. Nair, and William J. Welsh
pp 3257–3270Publication Date (Web): June 13, 2002 (Article)
DOI: 10.1021/jm0102811
N6-Alkyl-2-alkynyl Derivatives of Adenosine as Potent and Selective Agonists at the Human Adenosine A3 Receptor and a Starting Point for Searching A2B Ligands
Rosaria Volpini, Stefano Costanzi, Catia Lambertucci, Sara Taffi, Sauro Vittori, Karl-Norbert Klotz, and Gloria Cristalli
pp 3271–3279Publication Date (Web): June 18, 2002 (Article)
DOI: 10.1021/jm0109762
Synthesis and Pharmacological Testing of 1,2,3,4,10,14b-Hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and Its Enantiomers in Comparison with the Two Antidepressants Mianserin and Mirtazapine
Håkan V. Wikström, Marguérite M. Mensonides-Harsema, Thomas I. F. H. Cremers, Ejner K. Moltzen, and Jørn Arnt
pp 3280–3285Publication Date (Web): June 19, 2002 (Article)
DOI: 10.1021/jm010566d
Structure−Activity Relationships of Methoctramine-Related Polyamines as Muscular Nicotinic Receptor Noncompetitive Antagonists. 3.1 Effect of Inserting the Tetraamine Backbone into a Macrocyclic Structure
Maria L. Bolognesi, M. Gabriele Bixel, Gabriella Marucci, Manuela Bartolini, Michael Krauss, Piero Angeli, Alessandra Antonello, Michela Rosini, Vincenzo Tumiatti, Ferdinand Hucho, and Carlo Melchiorre
pp 3286–3295Publication Date (Web): June 14, 2002 (Article)
DOI: 10.1021/jm020835f
Structure−Activity Relationships on Phenylalanine-Containing Inhibitors of Histone Deacetylase: In Vitro Enzyme Inhibition, Induction of Differentiation, and Inhibition of Proliferation in Friend Leukemic Cells
Sybille Wittich, Hans Scherf, Changping Xie, Gerald Brosch, Peter Loidl, Clarissa Gerhäuser, and Manfred Jung
pp 3296–3309Publication Date (Web): June 20, 2002 (Article)
DOI: 10.1021/jm0208119
Rational Design and Synthesis of a Novel Thyroid Hormone Antagonist That Blocks Coactivator Recruitment
Ngoc-Ha Nguyen, James W. Apriletti, Suzana T. Cunha Lima, Paul Webb, John D. Baxter, and Thomas S. Scanlan
pp 3310–3320Publication Date (Web): June 19, 2002 (Article)
DOI: 10.1021/jm0201013
Brief Articles
Synthesis and Antiviral Activity of New Anti-HIV Amprenavir Bioisosteres
Luc Rocheblave, Frédéric Bihel, Céline De Michelis, Ghislaine Priem, Jérôme Courcambeck, Brice Bonnet, Jean-Claude Chermann, and Jean-Louis Kraus
pp 3321–3324Publication Date (Web): June 20, 2002 (Brief Article)
DOI: 10.1021/jm0208323
Book Reviews
Organic-Chemical Drugs and Their Synonyms. 8th Edition Edited by Martin Negwehr and Hans-Georg Scharnow. Wiley-VCH, Weinheim, Federal Republic of Germany. 2001. xvii + 4680 pp (in six volumes). 17 × 25 cm. ISBN 3-529-30247-6. $1435.00.
Joseph G. Cannon
p 3325Publication Date (Web): May 31, 2002 (Book Review)
DOI: 10.1021/jm0201868
Neurotransmitters, Drugs, and Brain Function Edited by R. A. Webster. John-Wiley & Sons, Ltd., Chichester, U.K. 2001. vi + 534 pp. 17 × 25 cm. ISBN 0-47197819-1. $145.00.
Roger M. Pinder
p 3325Publication Date (Web): June 4, 2002 (Book Review)
DOI: 10.1021/jm0201870
Anticancer Agents, Frontiers in Cancer Chemotherapy. ACS Symposium Series 796 Edited by Iwao Ojima, Gregory D. Vite, and Karl-Heinz Altman. American Chemical Society, Washington, DC. 2001. xii + 364 pp. 15.5 × 23.5 cm. ISBN 0-8412-3745-A. $140.00.
Kenneth G. Holden
pp 3325–3326Publication Date (Web): June 14, 2002 (Book Review)
DOI: 10.1021/jm0202223