Journal of Medicinal Chemistry
Volume 43, Issue 2 (January 27, 2000)
Copyright © 2000 American Chemical Society

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COMMUNICATIONS

139-141

Structural Determinants of Efficacy for Opioid Receptors in the Orvinol Series: 7,7-Spiro Analogues of Buprenorphine Stephen M. Husbands and John W. Lewis [Full Article - PDF]

142-145

Synthesis and Pharmacological Characterization of [125I]Iodomethyllycaconitine ([125I]Iodo-MLA). A New Ligand for the 7 Nicotinic Acetylcholine Receptor Hernán A. Navarro, Desong Zhong, Philip Abraham, Heng Xu, and F. Ivy Carroll [Full Article - PDF]

EXPEDITED ARTICLES

146-155

Structure-Based Discovery of Small Molecule Inhibitors Targeted to Protein Tyrosine Phosphatase 1B Mauro Sarmiento, Li Wu, Yen-Fang Keng, Li Song, Zhaowen Luo, Ziwei Huang, Guo-Zhang Wu, Adam K. Yuan, and Zhong-Yin Zhang [Full Article - PDF]

ARTICLES

156-166

Structure-Activity Relationships and Pharmacokinetic Analysis for a Series of Potent, Systemically Available Biphenylsulfonamide Matrix Metalloproteinase Inhibitors Patrick M. O'Brien, Daniel F. Ortwine, Alexander G. Pavlovsky, Joseph A. Picard, Drago R. Sliskovic, Bruce D. Roth, Richard D. Dyer, Linda L. Johnson, Chiu Fai Man, and Hussein Hallak [Full Article - PDF]

167-176

Antitumor Agents. 199. Three-Dimensional Quantitative Structure-Activity Relationship Study of the Colchicine Binding Site Ligands Using Comparative Molecular Field Analysis Shun-Xiang Zhang, Jun Feng, Sheng-Chu Kuo, Arnold Brossi, Ernest Hamel, Alexander Tropsha, and Kuo-Hsiung Lee [Full Article - PDF]

177-189

3,4-Dihydro-2(1H)-quinolinone as a Novel Antidepressant Drug: Synthesis and Pharmacology of 1-[3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and Its Derivatives Yasuo Oshiro, Yoji Sakurai, Seiji Sato, Nobuyuki Kurahashi, Tatsuyoshi Tanaka, Tetsuro Kikuchi, Katsura Tottori, Yasufumi Uwahodo, Takashi Miwa, and Takao Nishi [Full Article - PDF]

190-198

A Potential Melanoma Tracer: Synthesis, Radiolabeling, and Biodistribution in Mice of a New Nitridotechnetium Bis(aminothiol) Derivative Pharmacomodulated by a N-(Diethylaminoethyl)benzamide Philippe Auzeloux, Janine Papon, El Mostapha Azim, Michèle Borel, Roberto Pasqualini, Annie Veyre, and Jean-Claude Madelmont [Full Article - PDF]

199-204

Synthesis and in Vitro Anti-Mycobacterium Activity of N-Alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary Toxicity and Pharmacokinetic Evaluation Giuseppe Pagani, Massimo Pregnolato, Daniela Ubiali, Marco Terreni, Claudio Piersimoni, Francesco Scaglione, Franco Fraschini, Alicia Rodríguez Gascón, and José Luis Pedraz Muñoz [Full Article - PDF]

205-213

Novel 3-Aminomethyl- and 4-Aminopiperidine Analogues of 1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: Synthesis and Evaluation as Dopamine Transporter Ligands Sung-Woon Choi, David R. Elmaleh, Robert N. Hanson, and Alan J. Fischman [Full Article - PDF]

214-223

Synthesis and Biological Evaluation of 3,4-Diaryloxazolones: A New Class of Orally Active Cyclooxygenase-2 Inhibitors Carles Puig, María I. Crespo, Núria Godessart, Joan Feixas, Javier Ibarzo, Juan-Miguel Jiménez, Lídia Soca, Ignasi Cardelús, Ascensión Heredia, Montserrat Miralpeix, Jaume Puig, Jordi Beleta, Josep M. Huerta, Manel López, Victor Segarra, Hamish Ryder, and José M. Palacios [Full Article - PDF]

224-235

Synthesis and Evaluation of Hydroxylated Polyamine Analogues as Antiproliferatives Raymond J. Bergeron, Ralf Müller, Jörg Bussenius, James S. McManis, Ronald L. Merriman, Richard E. Smith, Hua Yao, and William R. Weimar [Full Article - PDF]

236-249

Secondary Amides of (R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionic Acid as Inhibitors of Pyruvate Dehydrogenase Kinase Thomas D. Aicher, Robert C. Anderson, Jiaping Gao, Suraj S. Shetty, Gary M. Coppola, James L. Stanton, Douglas C. Knorr, Donald M. Sperbeck, Leonard J. Brand, Christine C. Vinluan, Emma L. Kaplan, Carol J. Dragland, Hollis C. Tomaselli, Amin Islam, Robert J. Lozito, Xilin Liu, Wieslawa M. Maniara, William S. Fillers, Dominick DelGrande, R. Eric Walter, and William R. Mann [Full Article - PDF]

250-260

N-Cycloalkyl Derivatives of Adenosine and 1-Deazaadenosine as Agonists and Partial Agonists of the A1 Adenosine Receptor Sauro Vittori, Anna Lorenzen, Christina Stannek, Stefano Costanzi, Rosaria Volpini, Adriaan P. IJzerman, Jakobien K. Von Frijtag Drabbe Kunzel, and Gloria Cristalli [Full Article - PDF]

261-269

Esterase-Sensitive Nitric Oxide Donors of the Diazeniumdiolate Family: In Vitro Antileukemic Activity Joseph E. Saavedra, Paul J. Shami, Lai Yi Wang, Keith M. Davies, Melissa N. Booth, Michael L. Citro, and Larry K. Keefer [Full Article - PDF]

270-277

A Structure-Affinity Relationship Study on Derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a High-Affinity and Selective D4 Receptor Ligand Roberto Perrone, Francesco Berardi, Nicola A. Colabufo, Marcello Leopoldo, and Vincenzo Tortorella [Full Article - PDF]

278-282

Synthesis and Antiviral Activity of Novel Anti-VZV 5-Substituted Uracil Nucleosides with a Cyclopropane Sugar Moiety Tomoyuki Onishi, Chika Mukai, Ryusuke Nakagawa, Takaaki Sekiyama, Miho Aoki, Katsuya Suzuki, Harumi Nakazawa, Nobukazu Ono, Yuko Ohmura, Satoshi Iwayama, Masahiko Okunishi, and Takashi Tsuji [Full Article - PDF]

283-291

Structure-Function Relationships in Aminoquinolines: Effect of Amino and Chloro Groups on Quinoline-Hematin Complex Formation, Inhibition of -Hematin Formation, and Antiplasmodial Activity Timothy J. Egan, Roger Hunter, Catherine H. Kaschula, Helder M. Marques, Ashley Misplon, and Jason Walden [Full Article - PDF]

292-300

Carbonic Anhydrase Inhibitors: Synthesis of Membrane-Impermeant Low Molecular Weight Sulfonamides Possessing in Vivo Selectivity for the Membrane-Bound versus Cytosolic Isozymes Andrea Scozzafava, Fabrizio Briganti, Marc A. Ilies, and Claudiu T. Supuran [Full Article - PDF]

BOOK REVIEWS

301-301

Organic Reactions. Volume 54 Leo A. Paquette, Editor-in-Chief. John Wiley & Sons, Inc., New York. 1999. vii + 442 pp. 16 × 24 cm. ISBN 0-471-34888-0. $89.95. Jonathan P. Pease [Full Article - PDF]

302-302

Molecular Structure Description. The Electrotopological State By Lemont B. Kier and Lowell H. Hall. Forward by Gerald M. Maggiora. Academic Press, San Diego, CA. 1999. xx + 245 + 41 pp. 16 x 35 cm. ISBN 0-12-406555-4. $99.95. William J. Dunn III [Full Article - PDF]

ADDITIONS AND CORRECTIONS

303-303

Synthesis, Structure-Activity Relationships, and RAR-Ligand Interactions of Nitrogen Heteroarotinoids. Arindam Dhar, Shengquan Liu, Jozef Klucik, K. Darrell Berlin, Matora M. Madler, Shennan Lu, R. Todd Ivey, David Zacheis, Chad W. Brown, E. C. Nelson, Paul J. Birckbichler, and Doris M. Benbrook: [Full Article - PDF]

304-304

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]