Journal of Medicinal Chemistry
Volume 42, Issue 20 (October 7, 1999)
Copyright © 1999 American Chemical Society

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ANNOUNCEMENT

4015-4015

2000-2001 Predoctoral Fellowships [Full Article - PDF]

EXPEDITED ARTICLES

4016-4020

Diethylcarbamoylating/Nitroxylating Agents as Dual Action Inhibitors of Aldehyde Dehydrogenase: A Disulfiram-Cyanamide Merger Terry T. Conway, Eugene G. DeMaster, David J. W. Goon, Frances N. Shirota, and Herbert T. Nagasawa [Full Article - PDF]

ARTICLES

4021-4027

High-Resolution NMR and Computer Modeling Studies of the Cannabimimetic Aminoalkylindole Prototype WIN-55212-2 Xiang-Qun Xie, Xiu-Wen Han, Jian-Zhong Chen, Michael Eissenstat, and Alexandros Makriyannis [Full Article - PDF]

4028-4041

Design, Synthesis, and Evaluation of a Novel Sequence-Selective Epoxide-Containing DNA Cross-Linking Agent Based on the Pyrrolo[2,1-c][1,4]benzodiazepine System Stuart C. Wilson, Philip W. Howard, Stephen M. Forrow, John A. Hartley, Lesley J. Adams, Terence C. Jenkins, Lloyd R. Kelland, and David E. Thurston [Full Article - PDF]

4042-4053

Synthesis and Antiviral Activity of Ethidium-Arginine Conjugates Directed Against the TAR RNA of HIV-1 Valérie Peytou, Roger Condom, Nadia Patino, Roger Guedj, Anne-Marie Aubertin, Nathalie Gelus, Christian Bailly, Raphaël Terreux, and Daniel Cabrol-Bass [Full Article - PDF]

4054-4061

Inhibitors of the C2-Symmetric HIV-1 Protease: Nonsymmetric Binding of a Symmetric Cyclic Sulfamide with Ketoxime Groups in the P2/P2' Side Chains Johan Hultén, Hans O. Andersson, Wesley Schaal, Helena U. Danielson, Björn Classon, Ingemar Kvarnström, Anders Karlén, Torsten Unge, Bertil Samuelsson, and Anders Hallberg [Full Article - PDF]

4062-4070

A Novel Approach to Predicting P450 Mediated Drug Metabolism. CYP2D6 Catalyzed N-Dealkylation Reactions and Qualitative Metabolite Predictions Using a Combined Protein and Pharmacophore Model for CYP2D6 Marcel J. de Groot, Mark J. Ackland, Valerie A. Horne, Alexander A. Alex, and Barry C. Jones [Full Article - PDF]

4071-4080

Bioreductive Activation of a Series of Indolequinones by Human DT-Diaphorase: Structure-Activity Relationships Roger M. Phillips, Matthew A. Naylor, Mohammed Jaffar, Stephen W. Doughty, Steven A. Everett, Anthony G. Breen, Guzanfar A. Choudry, and Ian J. Stratford [Full Article - PDF]

4081-4087

Antitumor Agents. 196. Substituted 2-Thienyl-1,8-naphthyridin-4-ones: Their Synthesis, Cytotoxicity, and Inhibition of Tubulin Polymerization Shun-Xiang Zhang, Kenneth F. Bastow, Yoko Tachibana, Sheng-Chu Kuo, Ernest Hamel, Anthony Mauger, Ven L. Narayanan, and Kuo-Hsiung Lee [Full Article - PDF]

4088-4098

Discovery of Potent and Selective SH2 Inhibitors of the Tyrosine Kinase ZAP-70 Chi B. Vu, Evelyn G. Corpuz, Taylor J. Merry, Selvaluxmi G. Pradeepan, Catherine Bartlett, Regine S. Bohacek, Martyn C. Botfield, Charles J. Eyermann, Berkley A. Lynch, Ian A. MacNeil, Mary K. Ram, Marie Rose van Schravendijk, Shelia Violette, and Tomi K. Sawyer [Full Article - PDF]

4099-4107

Synthesis and Enantiopharmacology of New AMPA-Kainate Receptor Agonists Paola Conti, Marco De Amici, Giovambattista De Sarro, Milena Rizzo, Tine Bryan Stensbl, Hans Bräuner-Osborne, Ulf Madsen, Lucio Toma, and Carlo De Micheli [Full Article - PDF]

4108-4121

Inhibition of Neuronal Nitric Oxide Synthase by 4-Amino Pteridine Derivatives: Structure-Activity Relationship of Antagonists of (6R)-5,6,7,8-Tetrahydrobiopterin Cofactor Lothar G. Fröhlich, Peter Kotsonis, Hermann Traub, Shahriyar Taghavi-Moghadam, Najim Al-Masoudi, Heinrich Hofmann, Hartmut Strobel, Hans Matter, Wolfgang Pfleiderer, and Harald H. H. W. Schmidt [Full Article - PDF]

4122-4128

Design and Synthesis of Lipophilic Phosphoramidate d4T-MP Prodrugs Expressing High Potency Against HIV in Cell Culture: Structural Determinants for in Vitro Activity and QSAR Adam Q. Siddiqui, Christopher McGuigan, Carlo Ballatore, Fabio Zuccotto, Ian H. Gilbert, Erik De Clercq, and Jan Balzarini [Full Article - PDF]

4129-4139

Protein Kinase C Ligands Based on Tetrahydrofuran Templates Containing a New Set of Phorbol Ester Pharmacophores Jeewoo Lee, Ji-Hye Kang, Sang-Yoon Lee, Kee-Chung Han, Christina M. Torres, Dipak K. Bhattacharyya, Peter M. Blumberg, and Victor E. Marquez [Full Article - PDF]

4140-4149

Synthesis and Structure-Activity Relationships of the (Alkylamino)piperidine-Containing BHAP Class of Non-Nucleoside Reverse Transcriptase Inhibitors: Effect of 3-Alkylpyridine Ring Substitution Michael J. Genin, Toni J. Poel, Paul D. May, Laurice A. Kopta, Yoshihiko Yagi, Robert A. Olmsted, Janice M. Friis, Richard L. Voorman, Wade J. Adams, Richard C. Thomas, and Donna L. Romero [Full Article - PDF]

4150-4160

Urea-PETT Compounds as a New Class of HIV-1 Reverse Transcriptase Inhibitors. 3. Synthesis and Further Structure-Activity Relationship Studies of PETT Analogues Marita Högberg, Christer Sahlberg, Per Engelhardt, Rolf Noréen, Jussi Kangasmetsä, Nils Gunnar Johansson, Bo Öberg, Lotta Vrang, Hong Zhang, Britt-Louise Sahlberg, Torsten Unge, Seved Lövgren, Kerstin Fridborg, and Kristina Bäckbro [Full Article - PDF]

4161-4171

6-Substituted 2-Oxo-2H-1-benzopyran-3-carboxylic Acid as a Core Structure for Specific Inhibitors of Human Leukocyte Elastase Caroline Doucet, Lionel Pochet, Nicole Thierry, Bernard Pirotte, Jacques Delarge, and Michèle Reboud-Ravaux [Full Article - PDF]

4172-4184

Antitumor Benzothiazoles. 8. Synthesis, Metabolic Formation, and Biological Properties of the C- and N-Oxidation Products of Antitumor 2-(4-Aminophenyl)benzothiazoles Eiji Kashiyama, Ian Hutchinson, Mei-Sze Chua, Sherman F. Stinson, Lawrence R. Phillips, Gurmeet Kaur, Edward A. Sausville, Tracey D. Bradshaw, Andrew D. Westwell, and Malcolm F. G. Stevens [Full Article - PDF]

4185-4192

Design and Synthesis of Potent Bradykinin Agonists Containing a Benzothiazepine Moiety Muriel Amblard, Isabelle Daffix, Philippe Bedos, Gilbert Bergé, Didier Pruneau, Jean-Luc Paquet, Jean-Michel Luccarini, Pierre Bélichard, Pierre Dodey, and Jean Martinez [Full Article - PDF]

4193-4201

Synthesis and Characterization of Bradykinin B2 Receptor Agonists Containing Constrained Dipeptide Mimics Muriel Amblard, Isabelle Daffix, Gilbert Bergé, Monique Calmès, Pierre Dodey, Didier Pruneau, Jean-Luc Paquet, Jean-Michel Luccarini, Pierre Bélichard, and Jean Martinez [Full Article - PDF]

4202-4213

Synthesis and Antimicrobial Activity of 4H-4-Oxoquinolizine Derivatives: Consequences of Structural Modification at the C-8 Position Zhenkun Ma, Daniel T. W. Chu, Curt S. Cooper, Qun Li, Anthony K. L. Fung, Sanyi Wang, Linus L. Shen, Robert K. Flamm, Angela M. Nilius, Jeffery D. Alder, Jonathan A. Meulbroek, and Yat Sun Or [Full Article - PDF]

4214-4224

WB 4101-Related Compounds. 2. Role of the Ethylene Chain Separating Amine and Phenoxy Units on the Affinity for 1-Adrenoreceptor Subtypes and 5-HT1A Receptors Maria L. Bolognesi, Roberta Budriesi, Andrea Cavalli, Alberto Chiarini, Roberto Gotti, Amedeo Leonardi, Anna Minarini, Elena Poggesi, Maurizio Recanatini, Michela Rosini, Vincenzo Tumiatti, and Carlo Melchiorre [Full Article - PDF]

4225-4231

Heterodimeric Tacrine-Based Acetylcholinesterase Inhibitors: Investigating Ligand-Peripheral Site Interactions Paul R. Carlier, Ella S.-H. Chow, Yifan Han, Jing Liu, Jamal El Yazal, and Yuan-Ping Pang [Full Article - PDF]

4232-4238

Selective A3 Adenosine Receptor Antagonists: Water-Soluble 3,5-Diacyl-1,2,4-trialkylpyridinium Salts and Their Oxidative Generation from Dihydropyridine Precursors Rongyuan Xie, An-Hu Li, Xiao-Duo Ji, Neli Melman, Mark E. Olah, Gary L. Stiles, and Kenneth A. Jacobson [Full Article - PDF]

4239-4249

Synthesis of a Series of 4-Benzyloxyaniline Analogues as Neuronal N-Type Calcium Channel Blockers with Improved Anticonvulsant and Analgesic Properties Lain-Yen Hu, Todd R. Ryder, Michael F. Rafferty, M. Rose Feng, Susan M. Lotarski, David M. Rock, Michael Sinz, Sally J. Stoehr, Charles P. Taylor, Mark L. Weber, S. Scott Bowersox, George P. Miljanich, Elizabeth Millerman, Yong-Xiang Wang, and Balazs G. Szoke [Full Article - PDF]

4250-4256

3-Alkyl-6-Chloro-2-pyrones: Selective Inhibitors of Pancreatic Cholesterol Esterase Lorraine M. Deck, Miranda L. Baca, Stephanie L. Salas, Lucy A. Hunsaker, and David L. Vander Jagt [Full Article - PDF]

4257-4263

Further Studies on Oxygenated Tryptamines with LSD-like Activity Incorporating a Chiral Pyrrolidine Moiety into the Side Chain Madina Gerasimov, Danuta Marona-Lewicka, Deborah M. Kurrasch-Orbaugh, Amjad M. Qandil, and David E. Nichols [Full Article - PDF]

BRIEF ARTICLES

4264-4268

Preparation and Characterization of Novel trans-[PtCl2(amine)(isopropylamine)] Compounds: Cytotoxic Activity and Apoptosis Induction in ras-Transformed Cells Eva I. Montero, Sonia Díaz, Ana Ma González-Vadillo, José M. Pérez, C. Alonso, and Carmen Navarro-Ranninger [Full Article - PDF]

4269-4274

Novel Partial Agonists for the Histamine H3 Receptor with High in Vitro and in Vivo Activity Astrid Sasse, Holger Stark, Sibylle Reidemeister, Annette Hüls, Sigurd Elz, Xavier Ligneau, C. Robin Ganellin, Jean-Charles Schwartz, and Walter Schunack [Full Article - PDF]