Journal of Medicinal Chemistry
Volume 42, Issue 10 (May 20, 1999)
Copyright © 1999 American Chemical Society

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1683-1683

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ANNOUNCEMENTS

COMMUNICATIONS TO THE EDITOR

1684-1686

4-[[2-(1-Methyl-2-pyrrolidinyl)ethyl]thio]- phenol Hydrochloride (SIB-1553A): A Novel Cognitive Enhancer with Selectivity for Neuronal Nicotinic Acetylcholine Receptors Jean-Michel Vernier, Hassan El-Abdellaoui, Heather Holsenback, Nicholas D. P. Cosford, Leo Bleicher, Geoffrey Barker, Bruno Bontempi, Laura Chavez-Noriega, Frederique Menzaghi, Tadimeti S. Rao, Richard Reid, Aida I. Sacaan, Carla Suto, Mark Washburn, G. Kenneth Lloyd, and Ian A. McDonald [Full Article - PDF]

ARTICLES

1687-1697

Design, Synthesis, and in Vitro Activity of Catamphiphilic Reverters of Multidrug Resistance: Discovery of a Selective, Highly Efficacious Chemosensitizer with Potency in the Nanomolar Range Elisabetta Teodori, Silvia Dei, Patricia Quidu, Roberta Budriesi, Alberto Chiarini, Arlette Garnier-Suillerot, Fulvio Gualtieri, Dina Manetti, Maria Novella Romanelli, and Serena Scapecchi [Full Article - PDF]

1698-1704

Novel Arylpyrazino[2,3-c][1,2,6]thiadiazine 2,2-Dioxides as Inhibitors of Platelet Aggregation. 1. Synthesis and Pharmacological Evaluation Nuria Campillo, Concepción García, Pilar Goya, Juan A. Páez, Emilio Carrasco, and Manuel Grau [Full Article - PDF]

1705-1713

Solution Conformation of a Potent Cyclic Analogue of Tuftsin: Low- Temperature Nuclear Magnetic Resonance Study in a Cryoprotective Mixture Annamaria D'Ursi, Stefania Albrizio, Caterina Fattorusso, Antonio Lavecchia, Giancarlo Zanotti, and Piero A. Temussi [Full Article - PDF]

1714-1722

An Effort To Understand the Molecular Basis of Hypertension through the Study of Conformational Analysis of Losartan and Sarmesin Using a Combination of Nuclear Magnetic Resonance Spectroscopy and Theoretical Calculations Thomas Mavromoustakos, Antonios Kolocouris, Maria Zervou, Panagiota Roumelioti, John Matsoukas, and Rudiger Weisemann [Full Article - PDF]

1723-1738

Homology Modeling of Gelatinase Catalytic Domains and Docking Simulations of Novel Sulfonamide Inhibitors Ryuichi Kiyama, Yoshinori Tamura, Fumihiko Watanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani, and Mitsuaki Yodo [Full Article - PDF]

1739-1748

Molecular Hashkeys: A Novel Method for Molecular Characterization and Its Application for Predicting Important Pharmaceutical Properties of Molecules Anwar M. Ghuloum, Carleton R. Sage, and Ajay N. Jain [Full Article - PDF]

1749-1756

Design, Synthesis, and Activity of 2,6-Diphenoxypyridine-Derived Factor Xa Inhibitors Gary Phillips, David D. Davey, Keith A. Eagen, Sunil K. Koovakkat, Amy Liang, Howard P. Ng, Michael Pinkerton, Lan Trinh, Marc Whitlow, Alicia M. Beatty, and Michael M. Morrissey [Full Article - PDF]

1757-1766

Ligands for the Tyrosine Kinase p56lck SH2 Domain: Discovery of Potent Dipeptide Derivatives with Monocharged, Nonhydrolyzable Phosphate Replacements Pierre L. Beaulieu, Dale R. Cameron, Jean-Marie Ferland, Jean Gauthier, Elise Ghiro, James Gillard, Vida Gorys, Martin Poirier, Jean Rancourt, Dominik Wernic, and Montse Llinas-Brunet , Raj Betageri, Mario Cardozo, Eugene R. Hickey, Richard Ingraham, Scott Jakes, Alisa Kabcenell, Tom Kirrane, Susan Lukas, Usha Patel, John Proudfoot, Rajiv Sharma, Liang Tong, and Neil Moss [Full Article - PDF]

1767-1777

Extension of the Polyanionic Cosalane Pharmacophore as a Strategy for Increasing Anti-HIV Potency Mark Cushman, Shabana Insaf, Gitendra Paul, Jeffrey A. Ruell, Erik De Clercq, Dominique Schols, Christophe Pannecouque, Myriam Witvrouw, Catherine A. Schaeffer, Jim A. Turpin, Karen Williamson, and William G. Rice [Full Article - PDF]

1778-1788

The Role of Waters in Docking Strategies with Incremental Flexibility for Carbohydrate Derivatives: Heat-Labile Enterotoxin, a Multivalent Test Case Wendy E. Minke, David J. Diller, Wim G. J. Hol, and Christophe L. M. J. Verlinde [Full Article - PDF]

1789-1802

Structure-Activity Relationship of Small-Sized HIV Protease Inhibitors Containing Allophenylnorstatine Tsutomu Mimoto, Ryohei Kato, Haruo Takaku, Satoshi Nojima, Keisuke Terashima, Satoru Misawa, Tominaga Fukazawa, Takamasa Ueno, Hideharu Sato, Makoto Shintani, Yoshiaki Kiso, and Hideya Hayashi [Full Article - PDF]

1803-1815

Tyrosine Kinase Inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(Phenylamino)pyrido[d]pyrimidine Acrylamides as Irreversible Inhibitors of the ATP Binding Site of the Epidermal Growth Factor Receptor Jeff B. Smaill, Brian D. Palmer, Gordon W. Rewcastle, William A. Denny, Dennis J. McNamara, Ellen M. Dobrusin, Alexander J. Bridges, Hairong Zhou, H. D. Hollis Showalter, R. Thomas Winters, Wilbur R. Leopold, David W. Fry, James M. Nelson, Veronika Slintak, William L. Elliot, Billy J. Roberts, Patrick W. Vincent, and Sandra J. Patmore [Full Article - PDF]

1816-1822

Synthesis, Mode of Action, and Biological Activities of Rebeccamycin Bromo Derivatives Pascale Moreau, Fabrice Anizon, Martine Sancelme, Michelle Prudhomme, Danièle Sevère, Jean-François Riou, Jean-François Goossens, Jean-Pierre Hénichart, Christian Bailly, Emmanuel Labourier, Jamal Tazzi, Doriano Fabbro, Thomas Meyer, and A. M. Aubertin [Full Article - PDF]

1823-1827

A New Method for Rapidly Generating Inhibitors of Glyoxalase I inside Tumor Cells Using S-(N-Aryl-N-hydroxycarbamoyl)ethylsulfoxides Diana S. Hamilton, Malcolm J. Kavarana, Ellyn M. Sharkey, Julie L. Eiseman, and Donald J. Creighton [Full Article - PDF]

1828-1835

Studies on the Monoamine Oxidase-B-Catalyzed Biotransformation of 4-Azaaryl-1-methyl-1,2,3,6-tetrahydropyridine Derivatives Sandeep K. Nimkar, Stéphane Mabic, Andrea H. Anderson, Sonya L. Palmer, Thomas H. Graham, Milly de Jonge, Lisa Hazelwood, Sean J. Hislop, and Neal Castagnoli, Jr. [Full Article - PDF]

1836-1841

Syntheses of Biotinylated -Galactosylceramides and Their Effects on the Immune System and CD1 Molecules Teruyuki Sakai, Olga V. Naidenko, Hirosi Iijima, Mitchell Kronenberg, and Yasuhiko Koezuka [Full Article - PDF]

BRIEF ARTICLES

1842-1848

Synthesis and Evaluation of New Sulfur-Containing L-Arginine-Derived Inhibitors of Nitric Oxide Synthase Kohji Ichimori and Dennis J. Stuehr , Robert N. Atkinson and S. Bruce King [Full Article - PDF]

1849-1854

3-Amino-5-phenoxythiophenes: Syntheses and Structure-Function Studies of a Novel Class of Inhibitors of Cellular L-Triiodothyronine Uptake Detlef Briel, Dirk Pohlers, Mathias Uhlig, Silke Vieweg, Gerhard H. Scholz, Michael Thormann, and Hans-Jörg Hofmann [Full Article - PDF]

1855-1861

Synthesis of Novel Phenserine-Based-Selective Inhibitors of Butyrylcholinesterase for Alzheimer's Disease Qian-sheng Yu, Harold W. Holloway, Tadanobu Utsuki, Arnold Brossi, and Nigel H. Greig [Full Article - PDF]

BOOK REVIEWS

1862-1862

Smith and Williams' Introduction to the Principles of Drug Design and Action, 3rd Edition Edited by H. John Smith. Harwood Academic Publishers, Amsterdam. 1998. xiii + 454 pp. 17 x 25 cm. ISBN 90-5702-205-2. $30.00 (paperback) and $80.00 (cloth). Robert D. Sindelar [Full Article - PDF]