Journal of Medicinal Chemistry
Volume 41, Issue 23 (November 5, 1998)
Copyright © 1998 American Chemical Society

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COMMUNICATIONS TO THE EDITOR

4429-4432

TROTEC-1: A New High-Affinity Ligand for Labeling of the Dopamine Transporter Alexander Hoepping, Martina Reisgys, Peter Brust, Sepp Seifert, Hartmut Spies, Roger Alberto, and Bernd Johannsen [Full Article - PDF]

ARTICLES

4433-4438

Structure-Activity Relationships of a Series of Analogues of the Octadecaneuropeptide ODN on Calcium Mobilization in Rat Astrocytes Jérôme Leprince, Pierrick Gandolfo, Jean-Louis Thoumas, Christine Patte, Jean-Luc Fauchère, Hubert Vaudry, and Marie-Christine Tonon [Full Article - PDF]

4439-4452

Highly Potent Bisphosphonate Ligands for Phosphoglycerate Kinase David L. Jakeman, Andrew J. Ivory, Michael P. Williamson, and G. Michael Blackburn [Full Article - PDF]

4453-4465

Pharmacophoric Search and 3D-QSAR Comparative Molecular Field Analysis Studies on Agonists of Melatonin Sheep Receptors Christophe Marot, Philippe Chavatte, Luc Morin-Allory, Marie Claude Viaud, Gérald Guillaumet, Pierre Renard, Daniel Lesieur, and André Michel [Full Article - PDF]

4466-4474

Efficacious, Orally Bioavailable Thrombin Inhibitors Based on 3-Aminopyridinone or 3-Aminopyrazinone Acetamide Peptidomimetic Templates Philip E. J. Sanderson, Terry A. Lyle, Kellie J. Cutrona, Dona L. Dyer, Bruce D. Dorsey, Colleen M. McDonough, Adel M. Naylor-Olsen, I-Wu Chen, Zhongguo Chen, Jacquelynn J. Cook, Carolyn M. Cooper, Stephen J. Gardell, Timothy R. Hare, Julie A. Krueger, S. Dale Lewis, Jiunn H. Lin, Bobby J. Lucas, Jr., Elizabeth A. Lyle, Joseph J. Lynch, Jr., Maria T. Stranieri, Kari Vastag, Youwei Yan, Jules A. Shafer, and Joseph P. Vacca [Full Article - PDF]

4475-4485

Synthesis and Antitumor Activity of New Glycosides of Epipodophyllotoxin, Analogues of Etoposide, and NK 611 Laurent Daley, Yves Guminski, Pierre Demerseman, Anna Kruczynski, Chantal Etiévant, Thierry Imbert, Bridget T. Hill, and Claude Monneret [Full Article - PDF]

4486-4491

Modified Ibogaine Fragments: Synthesis and Preliminary Pharmacological Characterization of 3-Ethyl-5-phenyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]benzothiophenes Simon M. N. Efange, Deborah C. Mash, Anil B. Khare, and Quinjie Ouyang [Full Article - PDF]

4492-4501

Clavaric Acid and Steroidal Analogues as Ras- and FPP-Directed Inhibitors of Human Farnesyl-Protein Transferase Russell B. Lingham, Keith C. Silverman, Hiranthi Jayasuriya, B. Moon Kim, Suzanne E. Amo, Francine R. Wilson, Deborah J. Rew, Michael D. Schaber, James D. Bergstrom, Kenneth S. Koblan, Samuel L. Graham, Nancy E. Kohl, Jackson B. Gibbs, and Sheo B. Singh [Full Article - PDF]

4502-4520

FLEXS: A Method for Fast Flexible Ligand Superposition Christian Lemmen, Thomas Lengauer, and Gerhard Klebe [Full Article - PDF]

4521-4532

Three-Dimensional Quantitative Structure-Activity Relationship Study of the Cannabimimetic (Aminoalkyl)indoles Using Comparative Molecular Field Analysis Joong-Youn Shim, Elizabeth R. Collantes, and William J. Welsh , Babu Subramaniam and Allyn C. Howlett , Michael A. Eissenstat and Susan J. Ward [Full Article - PDF]

4533-4541

6-Substituted 2,4-Diaminopyrido[3,2-d]pyrimidine Analogues of Piritrexim as Inhibitors of Dihydrofolate Reductase from Rat Liver, Pneumocystis carinii, and Toxoplasma gondii and as Antitumor Agents Aleem Gangjee, Yuanming Zhu, and Sherry F. Queener [Full Article - PDF]

4542-4549

Alkoxypsoralens, Novel Nonpeptide Blockers of Shaker-Type K+ Channels: Synthesis and Photoreactivity Heike Wulff, Heiko Rauer, Tim Düring, Christine Hanselmann, Katharina Ruff, Anja Wrisch, Stephan Grissmer, and Wolfram Hänsel [Full Article - PDF]

4550-4555

Synthesis and Enzymic Evaluation of 4-Mercapto-6-oxo-1,4-azaphosphinane-2-carboxylic Acid 4-Oxide as an Inhibitor of Mammalian Dihydroorotase Michael K. Manthey, Danny T. C. Huang, William A. Bubb, and Richard I. Christopherson [Full Article - PDF]

4556-4566

Substituted Tetrahydropyrrolo[2,1-b]oxazol-5(6H)-ones and Tetrahydropyrrolo[2,1-b]thiazol-5(6H)-ones as Hypoglycemic Agents Thomas D. Aicher, Bork Balkan, Philip A. Bell, Leonard J. Brand, S. H. Cheon, Rhonda O. Deems, Jay B. Fell, William S. Fillers, James D. Fraser, Jiaping Gao, Douglas C. Knorr, Gerald G. Kahle, Christina L. Leone, Jeffrey Nadelson, Ronald Simpson, and Howard C. Smith [Full Article - PDF]

4567-4576

Use of Papain as a Model for the Structure-Based Design of Cathepsin K Inhibitors: Crystal Structures of Two Papain-Inhibitor Complexes Demonstrate Binding to S'-Subsites Judith M. LaLonde, Baoguang Zhao, Ward W. Smith, Cheryl A. Janson, Renee L. DesJarlais, Thaddeus A. Tomaszek, Thomas J. Carr, Scott K. Thompson, Hye-Ja Oh, Dennis S. Yamashita, Daniel F. Veber, and Sherin S. Abdel-Meguid [Full Article - PDF]

4577-4586

Structure-Based Enhancement of Boronic Acid-Based Inhibitors of AmpC -Lactamase G. Scott Weston, Jesús Blázquez, Fernando Baquero, and Brian K. Shoichet [Full Article - PDF]

4587-4598

A Novel Class of Orally Active Non-Peptide Bradykinin B2 Receptor Antagonists. 4. Discovery of Novel Frameworks Mimicking the Active Conformation Yoshito Abe, Hiroshi Kayakiri, Shigeki Satoh, Takayuki Inoue, Yuki Sawada, Noriaki Inamura, Masayuki Asano, Ichiro Aramori, Chie Hatori, Hiroe Sawai, Teruo Oku, and Hirokazu Tanaka [Full Article - PDF]

4599-4606

Novel Disaccharide Inhibitors of Human Glioma Cell Division Begoña Aguilera, Lorenzo Romero-Ramírez, José Abad-Rodríguez, Guillermo Corrales, Manuel Nieto-Sampedro, and Alfonso Fernández-Mayoralas [Full Article - PDF]

4607-4614

Structural Optimization Affording 2-(R)-(1-(R)-3,5-Bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist Jeffrey J. Hale, Sander G. Mills, Malcolm MacCoss, Paul E. Finke, Margaret A. Cascieri, Sharon Sadowski, Elzbieta Ber, Gary G. Chicchi, Marc Kurtz, Joseph Metzger, George Eiermann, Nancy N. Tsou, F. David Tattersall, Nadia M. J. Rupniak, Angela R. Williams, Wayne Rycroft, Richard Hargreaves, and D. Euan MacIntyre [Full Article - PDF]

4615-4622

2-Fluoro-4-pyridinylmethyl Analogues of Linopirdine as Orally Active Acetylcholine Release-Enhancing Agents with Good Efficacy and Duration of Action Richard A. Earl, Robert Zaczek, Christopher A. Teleha, Barbara N. Fisher, Carla M. Maciag, Maria E. Marynowski, Andrew R. Logue, S. William Tam, William J. Tinker, Shiew-Mei Huang, and Robert J. Chorvat [Full Article - PDF]

4623-4635

4,4-Disubstituted Piperidine High-Affinity NK1 Antagonists: Structure-Activity Relationships and in Vivo Activity Graeme I. Stevenson, Ian Huscroft, Angus M. MacLeod, Christopher J. Swain, Margaret A. Cascieri, Gary G. Chicchi, Michael I. Graham, Timothy Harrison, Fintan J. Kelleher, Marc Kurtz, Tamara Ladduwahetty, Kevin J. Merchant, Joseph M. Metzger, D. E. MacIntyre, Sharon Sadowski, Balbinder Sohal, and Andrew P. Owens [Full Article - PDF]

4636-4647

Abasic Analogues of TSAO-T as the First Sugar Derivatives That Specifically Inhibit HIV-1 Reverse Transcriptase Sonsoles Velázquez, Cristina Chamorro, María-Jesús Pérez-Pérez, Rosa Alvarez, María-Luisa Jimeno, Angel Martín-Domenech, Carlos Pérez, Federico Gago, Erik De Clercq, Jan Balzarini, Ana San-Félix, and María-José Camarasa [Full Article - PDF]

4648-4657

Anti-AIDS Agents. 34. Synthesis and Structure-Activity Relationships of Betulin Derivatives as Anti-HIV Agents I-Chen Sun, Hui-Kang Wang, Yoshiki Kashiwada, Jing-Kang Shen, L. Mark Cosentino, Chin-Ho Chen, Li-Ming Yang, and Kuo-Hsiung Lee [Full Article - PDF]

4658-4661

Synthesis and Cytotoxicity of 2-Acetyl-4,8-dihydrobenzodithiophene-4,8-dione Derivatives Yu-Hua Chao, Sheng-Chu Kuo, Chun-Hsiung Wu, Chun-Yann Lee, Anthony Mauger, I-Chen Sun, Susan L. Morris-Natschke, and Kuo-Hsiung Lee [Full Article - PDF]

4662-4674

New 1,25-Dihydroxy-19-norvitamin D3 Compounds of High Biological Activity: Synthesis and Biological Evaluation of 2-Hydroxymethyl, 2-Methyl, and 2-Methylene Analogues Rafal R. Sicinski, Jean M. Prahl, Connie M. Smith, and Hector F. DeLuca [Full Article - PDF]

BOOK REVIEWS

4675-4675

Computer Modeling of Chemical Reactions in Enzymes and Solutions By Arieh Warshel. John Wiley & Sons, Inc., New York, NY. 1997. xiv + 236 pp. 15.5 × 23.5 cm. ISBN 0-471-18440-3. $49.95. Emile M. Bellott [Full Article - PDF]

4675-4676

The Merck Index. Twelfth Edition on CD-ROM and User Guide By Janet E. Ash. Chapman-Hall, London, 1996. ISBN 0-412-75650-1. $299.95. Emile M. Bellott [Full Article - PDF]