Journal of Medicinal Chemistry
Volume 41, Issue 18 (August 27, 1998)
Copyright © 1998 American Chemical Society

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COMMUNICATIONS TO THE EDITOR

3303-3306

3-Deoxy-D-myo-inositol 1-Phosphate, 1-Phosphonate, and Ether Lipid Analogues as Inhibitors of Phosphatidylinositol-3-kinase Signaling and Cancer Cell Growth Lixin Qiao, Fajun Nan, Mark Kunkel, Alfred Gallegos, Garth Powis, and Alan P. Kozikowski [Full Article - PDF]

ARTICLES

3307-3313

Anticonvulsant Activity and Interactions with Neuronal Voltage-Dependent Sodium Channel of Analogues of Ameltolide Joseph Vamecq, Didier Lambert, Jacques H. Poupaert, Bernard Masereel, and James P. Stables [Full Article - PDF]

3314-3324

Can We Learn To Distinguish between "Drug-like" and "Nondrug-like" Molecules? Ajay, W. Patrick Walters, and Mark A. Murcko [Full Article - PDF]

3325-3329

A Scoring Scheme for Discriminating between Drugs and Nondrugs Jens Sadowski and Hugo Kubinyi [Full Article - PDF]

3330-3336

Synthesis and Antiallergic Activity of Dimethyl-2-(phenylcarbamoyl)ethylsulfonium p-Toluenesulfonate Derivatives Yukio Tada, Ichiro Yamawaki, Shuichi Ueda, Hiroshi Matsumoto, Naosuke Matsuura, Mitsugi Yasumoto, Akihide Koda, and Mikio Hori [Full Article - PDF]

3337-3346

Design and Synthesis of Brefeldin A Sulfide Derivatives as Prodrug Candidates with Enhanced Aqueous Solubilities Ankush B. Argade, Rajesh Devraj, Jeffrey A. Vroman, Rudiger D. Haugwitz, Melinda Hollingshead, and Mark Cushman [Full Article - PDF]

3347-3359

Synthesis, Physicochemical Properties, and Evaluation of N-Substituted-2-alkyl-3-hydroxy-4(1H)-pyridinones Bijaya L. Rai, Lotfollah S. Dekhordi, Hicham Khodr, Yi Jin, Zudong Liu, and Robert C. Hider [Full Article - PDF]

3360-3366

Structure-Activity Study of the Nociceptin(1-13)-NH2 N-Terminal Tetrapeptide and Discovery of a Nociceptin Receptor Antagonist Girolamo Calo', Remo Guerrini, Raffaella Bigoni, Anna Rizzi, Clementina Bianchi, Domenico Regoli, and Severo Salvadori [Full Article - PDF]

3367-3372

4-Benzylamino-1-chloro-6-substituted Phthalazines: Synthesis and Inhibitory Activity toward Phosphodiesterase 5 Nobuhisa Watanabe, Yasuhiro Kabasawa, Yasutaka Takase, Masayuki Matsukura, Kazuki Miyazaki, Hiroki Ishihara, Kohtarou Kodama, and Hideyuki Adachi [Full Article - PDF]

3373-3386

Conformational Analysis of Ketolide, Conformations of RU 004 in Solution and Bound to Bacterial Ribosomes Gildas Bertho, Josyane Gharbi-Benarous, Marcel Delaforge, Catherine Lang, Annick Parent, and Jean-Pierre Girault [Full Article - PDF]

3387-3401

New Aza-Dipeptide Analogues as Potent and Orally Absorbed HIV-1 Protease Inhibitors: Candidates for Clinical Development Guido Bold, Alexander Fässler, Hans-Georg Capraro, Robert Cozens, Thomas Klimkait, Janis Lazdins, Jürgen Mestan, Bernard Poncioni, Johannes Rösel, David Stover, Marina Tintelnot-Blomley, Figan Acemoglu, Werner Beck, Eugen Boss, Martin Eschbach, Thomas Hürlimann, Elvira Masso, Serge Roussel, Katharina Ucci-Stoll, Dominique Wyss, and Marc Lang [Full Article - PDF]

3402-3408

Synthesis of 9-Deoxo-4''-deoxy-6,9-epoxyerythromycin Derivatives: Novel and Acid-Stable Motilides Ramin Faghih, Paul A. Lartey, Hugh N. Nellans, Louis Seif, Cynthia Burnell-Curty, Larry L. Klein, Paul Thomas, Albert Petersen, Anthony Borre, Thomas Pagano, Ki Hwan Kim, Matthew Heindel, Youssef L. Bennani, and Jacob J. Plattner [Full Article - PDF]

3409-3416

3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: A New Class of AMPA Receptor Antagonists Alba Chimirri, Giovambattista De Sarro, Angela De Sarro, Rosaria Gitto, Silvana Quartarone, Maria Zappalà, Andrew Constanti, and Vincenzo Libri [Full Article - PDF]

3417-3425

Small Molecular Probes for G-Protein-Coupled C5a Receptors: Conformationally Constrained Antagonists Derived from the C Terminus of the Human Plasma Protein C5a Allan K. Wong, Angela M. Finch, Gregory K. Pierens, David J. Craik, Stephen M. Taylor, and David P. Fairlie [Full Article - PDF]

3426-3434

Structure-Based Design and Synthesis of Lipophilic 2,4-Diamino-6-Substituted Quinazolines and Their Evaluation as Inhibitors of Dihydrofolate Reductases and Potential Antitumor Agents Aleem Gangjee, Anup P. Vidwans, Anil Vasudevan, Sherry F. Queener, Roy L. Kisliuk, Vivian Cody, Ruming Li, Nikolai Galitsky, Joe R. Luft, and Walter Pangborn [Full Article - PDF]

3435-3441

Synthesis and Evaluation of 2-Amino-9-(3-hydroxymethyl-4-alkoxycarbonyloxybut-1-yl)purines as Potential Prodrugs of Penciclovir Dae-Kee Kim, Namkyu Lee, Young-Woo Kim, Kieyoung Chang, Jae-Sun Kim, Guang-Jin Im, Won-Son Choi, Inho Jung, Taek-Soo Kim, Yong-Youn Hwang, Dong-Sun Min, Key An Um, Yong-Baik Cho, and Key H. Kim [Full Article - PDF]

3442-3449

Structure-Based Design and Synthesis of High Affinity Tripeptide Ligands of the Grb2-SH2 Domain Pascal Furet, Brigitte Gay, Giorgio Caravatti, Carlos García-Echeverría, Joseph Rahuel, Joseph Schoepfer, and Heinz Fretz [Full Article - PDF]

3450-3460

-Amino-thiols Inhibit the Zinc Metallopeptidase Activity of Tetanus Toxin Light Chain Loïc Martin, Fabrice Cornille, Pascale Coric, Bernard P. Roques, and Marie-Claude Fournié-Zaluski [Full Article - PDF]

3461-3466

Discovery and Preliminary SAR Studies of a Novel, Nonsteroidal Progesterone Receptor Antagonist Pharmacophore Charlotte L. F. Pooley, James P. Edwards, Mark E. Goldman, Ming-Wei Wang, Keith B. Marschke, Diane L. Crombie, and Todd K. Jones [Full Article - PDF]

3467-3476

Tipranavir (PNU-140690): A Potent, Orally Bioavailable Nonpeptidic HIV Protease Inhibitor of the 5,6-Dihydro-4-hydroxy-2-pyrone Sulfonamide Class Steve R. Turner, Joseph W. Strohbach, Ruben A. Tommasi, Paul A. Aristoff, Paul D. Johnson, Harvey I. Skulnick, Lester A. Dolak, Eric P. Seest, Paul K. Tomich, Michael J. Bohanon, Miao-Miao Horng, Janet C. Lynn, Kong-Teck Chong, Roger R. Hinshaw, Keith D. Watenpaugh, Musiri N. Janakiraman, and Suvit Thaisrivongs [Full Article - PDF]

3477-3492

Studies of Structure-Activity Relationship of Nitroxide Free Radicals and Their Precursors as Modifiers Against Oxidative Damage Murali C. Krishna, William DeGraff, Olga H. Hankovszky, Cecília P. Sár, Tamás Kálai, József Jeko, Angelo Russo, James B. Mitchell, and Kálmán Hideg [Full Article - PDF]

3493-3498

3-Alkyl Ethers of Clocinnamox: Delayed Long-Term -Antagonists with Variable Efficacy Stephen M. Husbands, John Sadd, Jillian H. Broadbear, James H. Woods, Jason Martin, John R. Traynor, Mario D. Aceto, Edward R. Bowman, Louis S. Harris, and John W. Lewis [Full Article - PDF]

3499-3506

Structure-Activity Relationships for a Series of Bis(phenylalkyl)amines: Potent Subtype-Selective Inhibitors of N-Methyl-D-aspartate Receptors Amir P. Tamiz, Edward R. Whittemore, Zhang-Lin Zhou, Jin-Cheng Huang, John A. Drewe, Jie-Cheng Chen, Sui-Xiong Cai, Eckard Weber, Richard M. Woodward, and John F. W. Keana [Full Article - PDF]

3507-3514

Synthesis and Biological Activity of Conformationally Restricted Analogues of Milnacipran: (1S,2R)-1-Phenyl-2-[(R)-1-amino-2-propynyl]-N,N- diethylcyclopropanecarboxamide Is a Novel Class of NMDA Receptor Channel Blocker Satoshi Shuto, Shizuka Ono, Hiroaki Imoto, Kiyonori Yoshii, and Akira Matsuda [Full Article - PDF]

3515-3529

New Cyclooxygenase-2/5-Lipoxygenase Inhibitors. 3. 7-tert-Butyl-2,3-dihydro-3,3-dimethylbenzofuran Derivatives as Gastrointestinal Safe Antiinflammatory and Analgesic Agents: Variations at the 5 Position John M. Janusz, Patricia A. Young, James M. Ridgeway, Michael W. Scherz, Kevin Enzweiler, Laurence I. Wu, Lixian Gan, Julian Chen, David E. Kellstein, Shelley A. Green, Jennifer L. Tulich, Theresa Rosario-Jansen, I. Jack Magrisso, Kenneth R. Wehmeyer, Deborah L. Kuhlenbeck, Thomas H. Eichhold, and Roy L. M. Dobson [Full Article - PDF]

3530-3538

Pyrazole Bioisosteres of Leflunomide as B-Cell Immunosuppressants for Xenotransplantation and Chronic Rejection: Scope and Limitations Christos Papageorgiou, Rainer Albert, Philipp Floersheim, Michel Lemaire, Francis Bitch, Hans-Peter Weber, Elsebeth Andersen, Valerie Hungerford, and Max H. Schreier [Full Article - PDF]

NOTES

3539-3545

Synthesis and Biological Activity of 4-Amino-7-oxo-Substituted Analogues of 5-Deaza-5,6,7,8-tetrahydrofolic Acid and 5,10-Dideaza-5,6,7,8-tetrahydrofolic Acid José I. Borrell, Jordi Teixidó, Blanca Martínez-Teipel, Josep Lluís Matallana, M. Teresa Copete, Ana Llimargas, and Eva García [Full Article - PDF]

3546-3549

Physical Parameters and Biological Stability of Yttrium(III) Diethylenetriaminepentaacetic Acid Derivative Conjugates Thomas J. McMurry, C. Greg Pippin, Chuanchu Wu, Kim A. Deal, Martin W. Brechbiel, Saed Mirzadeh, and Otto A. Gansow [Full Article - PDF]

BOOK REVIEWS

3550-3550

Methods in Molecular Biology, Volume 87. Combinatorial Peptide Library Protocols Edited by Shmuel Cabilly. Humana Press, Totowa, NJ. 1998. xiii + 313 pp. 15.5 × 23.5 cm. ISBN 0-89603-392-9. $74.50. Bruce A. Beutel [Full Article - PDF]

3550-3550

The P2 Nucleotide Receptors Edited by John T. Turner, Gary A. Weisman, and Jeffrey S. Fedan. Humana Press, Totowa, NJ. 1997. xi + 440 pp. 16 × 23.5 cm. ISBN 0-89603-425-9. $139.00. Shripad S. Bhagwat [Full Article - PDF]