Journal of Medicinal Chemistry
Volume 41, Issue 16 (July 30, 1998)
Copyright © 1998 American Chemical Society

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PERSPECTIVE

2911-2927

G-Protein Coupled Receptors: Models, Mutagenesis, and Drug Design Jack Andrew Bikker, Susanne Trumpp-Kallmeyer, and Christine Humblet [Full Article - PDF]

COMMUNICATIONS TO THE EDITOR

2928-2931

Discovery and Preclinical Pharmacology of a Novel, Potent, Nonsteroidal Estrogen Receptor Agonist/Antagonist, CP-336156, a Diaryltetrahydronaphthalene Robert L. Rosati, Paul Da Silva Jardine, Kimberly O. Cameron, David D. Thompson, Hua Zhu Ke, Steven M. Toler, Thomas A. Brown, Lydia C. Pan, Charles F. Ebbinghaus, Anthony R. Reinhold, Nancy C. Elliott, Bradley N. Newhouse, Christina M. Tjoa, Paul M. Sweetnam, Mark J. Cole, Mark W. Arriola, Jeffrey W. Gauthier, D. Todd Crawford, David F. Nickerson, Christine M. Pirie, Hong Qi, Hollis A. Simmons, and George T. Tkalcevic [Full Article - PDF]

2932-2933

3,6-Diamino-10-methylacridan: Uncharged Precursor of Acriflavine and Its Unique Antimicrobial Activity Jan Adamus, Jerzy Gbicki, Ireneusz Ciebiada, Ewa Korczak, and Andrzej Denys [Full Article - PDF]

2934-2938

Indole-2-carboxamide Inhibitors of Human Liver Glycogen Phosphorylase Dennis J. Hoover, Sheri Lefkowitz-Snow, Jana L. Burgess-Henry, William H. Martin, Sandra J. Armento, Ingrid A. Stock, R. Kirk McPherson, Paul E. Genereux, E. Michael Gibbs, and Judith L. Treadway [Full Article - PDF]

EXPEDITED ARTICLES

2939-2945

Substituted Salicylanilides as Inhibitors of Two-Component Regulatory Systems in Bacteria Mark J. Macielag, James P. Demers, Stephanie A. Fraga-Spano, Dennis J. Hlasta, Sigmond G. Johnson, Ramesh M. Kanojia, Ronald K. Russell, Zhihua Sui, Michele A. Weidner-Wells, Harvey Werblood, Barbara D. Foleno, Raul M. Goldschmidt, Michael J. Loeloff, Glenda C. Webb, and John F. Barrett [Full Article - PDF]

ARTICLES

2946-2959

4H-1,2,4-Pyridothiadiazine 1,1-Dioxides and 2,3-Dihydro-4H-1,2,4-pyridothiadiazine 1,1-Dioxides Chemically Related to Diazoxide and Cyclothiazide as Powerful Positive Allosteric Modulators of (R/S)-2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid Receptors: Design, Synthesis, Pharmacology, and Structure-Activity Relationships Bernard Pirotte, Tchao Podona, Ousmane Diouf, Pascal de Tullio, Philippe Lebrun, Léon Dupont, Fabian Somers, Jacques Delarge, Philippe Morain, Pierre Lestage, Jean Lepagnol, and Michael Spedding [Full Article - PDF]

2960-2971

Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 7. 8-Arylethyldipyridodiazepinones as Potent Broad-Spectrum Inhibitors of Wild-Type and Mutant Enzymes Janice M. Klunder, MaryAnn Hoermann, Charles L. Cywin, Eva David, Janice R. Brickwood, Racheline Schwartz, Kevin J. Barringer, Daniel Pauletti, Cheng-Kon Shih, David A. Erickson, Christopher L. Sorge, David P. Joseph, Susan E. Hattox, Julian Adams, and Peter M. Grob [Full Article - PDF]

2972-2984

Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 8. 8-Aryloxymethyl- and 8-Arylthiomethyldipyridodiazepinones Charles L. Cywin, Janice M. Klunder,,2 MaryAnn Hoermann, Janice R. Brickwood, Eva David,,3 Peter M. Grob, Racheline Schwartz, Daniel Pauletti, Kevin J. Barringer, Cheng-Kon Shih, Christopher L. Sorge, David A. Erickson, David P. Joseph, and Susan E. Hattox [Full Article - PDF]

2985-2993

Synthesis and Pharmacological Activity of Triazolo[1,5-a]triazine Derivatives Inhibiting Eosinophilia Fumihiko Akahoshi, Shinji Takeda, Takehiro Okada, Masahiko Kajii, Hiroko Nishimura, Masanori Sugiura, Yoshihisa Inoue, Chikara Fukaya, Youichiro Naito, Takashi Imagawa, and Norifumi Nakamura [Full Article - PDF]

2994-3000

Antiviral Activities of Methylated Nordihydroguaiaretic Acids. 1. Synthesis, Structure Identification, and Inhibition of Tat-Regulated HIV Transactivation Jih Ru Hwu, Wen Nan Tseng, John Gnabre, Paul Giza, and Ru Chih C. Huang [Full Article - PDF]

3001-3007

Antiviral Activities of Methylated Nordihydroguaiaretic Acids. 2. Targeting Herpes Simplex Virus Replication by the Mutation Insensitive Transcription Inhibitor Tetra-O-methyl-NDGA Hongshan Chen, Li Teng, Jian-Nong Li, Richard Park, David E. Mold, John Gnabre, Jih Ru Hwu, Wen Nan Tseng, and Ru Chih C. Huang [Full Article - PDF]

3008-3014

Noncalcemic, Antiproliferative, Transcriptionally Active, 24-Fluorinated Hybrid Analogues of the Hormone 1,25-Dihydroxyvitamin D3. Synthesis and Preliminary Biological Evaluation Gary H. Posner, Jae Kyoo Lee, Qiang Wang, Sara Peleg, Martin Burke, Henry Brem, Patrick Dolan, and Thomas W. Kensler [Full Article - PDF]

3015-3021

Benzoxazole Derivatives as Novel 5-HT3 Receptor Partial Agonists in the Gut Yasuo Sato, Megumi Yamada, Satoshi Yoshida, Tomoko Soneda, Midori Ishikawa, Tetsutaro Nizato, Kokichi Suzuki, and Fukio Konno [Full Article - PDF]

3022-3032

Novel Combretastatin Analogues Effective against Murine Solid Tumors: Design and Structure-Activity Relationships Koji Ohsumi, Ryusuke Nakagawa, Yumiko Fukuda, Toshihiro Hatanaka, Yoshihiro Morinaga, Yukio Nihei, Kazuo Ohishi, Yasuyo Suga, Yukio Akiyama, and Takashi Tsuji [Full Article - PDF]

3033-3040

A New Approach to the Design of Novel Inhibitors of Na+,K+-ATPase: 17-Substituted Seco-D 5-Androstane as Cassaine Analogues Sergio De Munari, Paolo Barassi, Alberto Cerri, Giorgio Fedrizzi, Mauro Gobbini, Massimo Mabilia, and Piero Melloni [Full Article - PDF]

3041-3047

Bis-Substituted Malonic Acid Hydroxamate Derivatives as Inhibitors of Human Neutrophil Collagenase (MMP8) Erich Graf von Roedern, Hans Brandstetter, Richard A. Engh, Wolfram Bode, Frank Grams, and Luis Moroder [Full Article - PDF]

3048-3061

Design, Synthesis, and Pharmacological Evaluation of Conformationally Constrained Analogues of N,N'-Diaryl- and N-Aryl-N-aralkylguanidines as Potent Inhibitors of Neuronal Na+ Channels Michel C. Maillard, Michael E. Perlman, Oved Amitay, Deborah Baxter, David Berlove, Sonia Connaughton, James B. Fischer, Jun Qing Guo, Lain-Yen Hu, Robert N. McBurney, Peter I. Nagy, Katragadda Subbarao, Elizabeth A. Yost, Lu Zhang, and Graham J. Durant [Full Article - PDF]

3062-3077

Synthesis and Structure-Activity Relationships of 2-Pyrazinylcarboxamido- benzoates and -Ionylideneacetamidobenzoates with Retinoidal Activity Paul Jones, Gérald B. Villeneuve, Chengpei Fei, Josie DeMarte, Allison J. Haggarty, Khin Than Nwe, Deborah A. Martin, Anne-Marie Lebuis, Joshua M. Finkelstein, Barbara J. Gour-Salin, Tak Hang Chan, and Brian R. Leyland-Jones [Full Article - PDF]

3078-3083

Discovery of Type II (Covalent) Inactivation of S-Adenosyl-L-homocysteine Hydrolase Involving Its "Hydrolytic Activity": Synthesis and Evaluation of Dihalohomovinyl Nucleoside Analogues Derived from Adenosine Stanislaw F. Wnuk, Yue Mao, Chong-Sheng Yuan, Ronald T. Borchardt, Graciela Andrei, Jan Balzarini, Erik De Clercq, and Morris J. Robins [Full Article - PDF]

3084-3090

Rational Design of Antitumor Prostaglandins with High Biological Stability Masaaki Suzuki, Toshihiro Kiho, Keiichiro Tomokiyo, Kyoji Furuta, Shoji Fukushima, Yoshikazu Takeuchi, Makoto Nakanishi, and Ryoji Noyori [Full Article - PDF]

3091-3098

Synthesis of 7-Arylmorphinans. Probing the "Address" Requirements for Selectivity at Opioid Receptors Peng Gao, Dennis L. Larson, and Philip S. Portoghese [Full Article - PDF]

BOOK REVIEWS

3099-3099

Principles of Process Research and Chemical Development in the Pharmaceutical Industry By Oljan Repic. John Wiley & Sons, New York. 1998. xvi + 213 pp. 16 × 24 cm. ISBN 0-471-16516-6. $74.95. Pat N. Confalone [Full Article - PDF]

3099-3100

Glycoanalysis Protocols Edited by Elizabeth F. Hounsell. Humana Press, Totowa, NJ. 1997. x + 262 pp. 15.5 × 23.5 cm. ISBN 0-896-0335-4. $64.50. Robert J. Linhardt [Full Article - PDF]

3100-3100

Pharmacology of Antimuscarinic Agents By Laszlo Gyermek. CRC Press, Boca Raton, FL. 1997. xx + 501 pp. 16 × 24 cm. ISBN 0-8493-8559-8. $129.95. B. V. Rama Sastry [Full Article - PDF]

3100-3101

Approaches to Design and Synthesis of Antiparasitic Drugs By Satyavan Sharma. Edited by Nitya Anand. Elsevier Science B.V., Amsterdam. 1997. xi + 511 pp. 17 × 25 cm. ISBN 0-444-89476-4. $265.75. Jonathan L. Vennerstrom [Full Article - PDF]

ADDITIONS AND CORRECTIONS

3102-3102

Synthesis and Anticonvulsant Activity of 2(3H)-Benzoxazolone and 2(3H)-Benzothiazolone Derivatives Huseyin Ucar, Kim Van derpoorten, Silvia Cacciaguerra, Santi Spampinato, James P. Stables, Paul Depovere, Majed Isa, Bernard Masereel, Jacques Delarge, and Jacques H. Poupaert [Full Article - PDF]

3102-3102

New Cyclooxygenase-2/5-Lipoxygenase Inhibitors. 2. 7-tert-Butyl-2,3-dihydro-3,3-dimethylbenzofuran Derivatives as Gastrointestinal Safe Antiinflammatory and Analgesic Agents: Variations of the Dihydrobenzofuran Ring John M. Janusz, Patricia A. Young, Michael W. Scherz, Kevin Enzweiler, Laurence I. Wu, Lixian Gan, Stanislaw Pikul, Kelly L. McDow-Dunham, Carl R. Johnson, C. B. Senanayake, 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]