Journal of Medicinal Chemistry
Volume 43, Issue 26 (December 28, 2000)
Copyright © 2000 American Chemical Society

Click [Full Article - PDF] to display or print the full article page image in PDF. Note: As of August 2000, Acrobat Reader 4.0 or later is recommended for PDFs.  

COMMUNICATIONS

4923-4926

4-Aryl-2,4-dioxobutanoic Acid Inhibitors of HIV-1 Integrase and Viral Replication in Cells John S. Wai, Melissa S. Egbertson, Linda S. Payne, Thorsten E. Fisher, Mark W. Embrey, Lekhanh O. Tran, Jeffrey Y. Melamed, H. Marie Langford, James P. Guare, Jr., Linghang Zhuang, Vanessa E. Grey, Joseph P. Vacca, M. Katharine Holloway, Adel M. Naylor-Olsen, Daria J. Hazuda, Peter J. Felock, Abigail L. Wolfe, Kara A. Stillmock, William A. Schleif, Lori J. Gabryelski, and Steven D. Young [Full Article - PDF]

4927-4929

Design and Synthesis of New Orally Active Nonpeptidic Inhibitors of Human Neutrophil Elastase Kazuyuki Ohmoto, Tetsuya Yamamoto, Toshihide Horiuchi, Hirotoshi Imanishi, Yoshihiko Odagaki, Kazuhito Kawabata, Tomohiko Sekioka, Yasushi Hirota, Shozo Matsuoka, Hisao Nakai, and Masaaki Toda , John C. Cheronis , Lyle W. Spruce , Albert Gyorkos , Maciej Wieczorek [Full Article - PDF]

4930-4933

A Novel Class of Potent 3-Isoxazolol GABAA Antagonists: Design, Synthesis, and Pharmacology Bente Frlund, Lena Tagmose, Tommy Liljefors, Tine Bryan Stensbl, Christine Engblom, Uffe Kristiansen, and Povl Krogsgaard-Larsen [Full Article - PDF]

ARTICLES

4934-4947

Pyrazole Ligands: Structure-Affinity/Activity Relationships and Estrogen Receptor--Selective Agonists Shaun R. Stauffer, Christopher J. Coletta, Rosanna Tedesco, Gisele Nishiguchi, Kathryn Carlson, Jun Sun, Benita S. Katzenellenbogen, and John A. Katzenellenbogen [Full Article - PDF]

4948-4963

Development of New Hydroxamate Matrix Metalloproteinase Inhibitors Derived from Functionalized 4-Aminoprolines Michael G. Natchus, Roger G. Bookland, Biswanath De, Neil G. Almstead, Stanislaw Pikul, Michael J. Janusz, Sandra A. Heitmeyer, Erin B. Hookfin, Lily C. Hsieh, Martin E. Dowty, Charles R. Dietsch, Vikram S. Patel, Susan M. Garver, Fei Gu, Matthew E. Pokross, Glen E. Mieling, Timothy R. Baker, David J. Foltz, Sean X. Peng, David M. Bornes, Michael J. Strojnowski, and Yetunde O. Taiwo [Full Article - PDF]

4964-4972

A Novel Series of 4-Piperidinopyridine and 4-Piperidinopyrimidine Inhibitors of 2,3-Oxidosqualene Cyclase-Lanosterol Synthase George R. Brown, David M. Hollinshead, Elaine S. E. Stokes, David Waterson, David S. Clarke, Alan J. Foubister, Steven C. Glossop, Fergus McTaggart, Donald J. Mirrlees, Graham J. Smith, and Robin Wood [Full Article - PDF]

4973-4980

Fluorosulfonyl-Substituted Xanthines as Selective Irreversible Antagonists for the A1-Adenosine Receptor Anthony R. Beauglehole, Stephen P. Baker, and Peter J. Scammells [Full Article - PDF]

4981-4992

Slow-Onset, Long-Duration 3-(3',4'-Dichlorophenyl)-1-indanamine Monoamine Reuptake Blockers as Potential Medications To Treat Cocaine Abuse Mark Froimowitz, Kuo-Ming Wu, Adel Moussa, Reem M. Haidar, Jurjus Jurayj, Clifford George, and Eliot L. Gardner [Full Article - PDF]

4993-4997

Highly Potent and Selective Inhibition of Varicella-Zoster Virus by Bicyclic Furopyrimidine Nucleosides Bearing an Aryl Side Chain Christopher McGuigan, Hubert Barucki, Sally Blewett, Antonella Carangio, Jonathan T. Erichsen, Graciela Andrei, Robert Snoeck, Erik De Clercq, and Jan Balzarini [Full Article - PDF]

4998-5002

D-Amino Acid Scan of -Melanocyte-Stimulating Hormone: Importance of Trp8 on Human MC3 Receptor Selectivity Paolo Grieco, Preeti M. Balse, David Weinberg, Tanya MacNeil, and Victor J. Hruby [Full Article - PDF]

5003-5009

5-Azidoimidacloprid and an Acyclic Analogue as Candidate Photoaffinity Probes for Mammalian and Insect Nicotinic Acetylcholine Receptors Shinzo Kagabu, Peter Maienfisch, Aiguo Zhang, Joaquin Granda-Minones, Joerg Haettenschwiler, Hartmut Kayser, Thomas Maetzke, and John E. Casida [Full Article - PDF]

5010-5016

Synthesis and Biological Activity of a Novel, Highly Potent Progesterone Receptor Antagonist Ulrike Fuhrmann, Holger Hess-Stumpp, Arwed Cleve, Günter Neef, Wolfgang Schwede, Jens Hoffmann, Karl-Heinrich Fritzemeier, and Kristof Chwalisz [Full Article - PDF]

5017-5029

A Potent, Long-Acting, Orally Active (2R)-2-[(1R)-3,3-Difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: A Novel Muscarinic M3 Receptor Antagonist with High Selectivity for M3 over M2 Receptors Morihiro Mitsuya, Kensuke Kobayashi, Kumiko Kawakami, Atsushi Satoh, Yoshio Ogino, Taro Kakikawa, Norikazu Ohtake, Toshifumi Kimura, Hiroyasu Hirose, Akio Sato, Tomosige Numazawa, Takuro Hasegawa, Kazuhito Noguchi, and Toshiaki Mase [Full Article - PDF]

5030-5036

Synthesis and in Vitro and in Vivo Activity of (-)-(1R,5R,9R)- and (+)-(1S,5S,9S)-N-Alkenyl-, -N-Alkynyl-, and -N-Cyanoalkyl-5,9-dimethyl-2'-hydroxy-6,7-benzomorphan Homologues Everette L. May, Arthur E. Jacobson, Mariena V. Mattson, John R. Traynor, James H. Woods, Louis S. Harris, Edward R. Bowman, and Mario D. Aceto [Full Article - PDF]

5037-5043

Optimization of Substituted N-3-Benzylimidazoquinazolinone Sulfonamides as Potent and Selective PDE5 Inhibitors David P. Rotella, Zhong Sun, Yeheng Zhu, John Krupinski, Ronald Pongrac, Laurie Seliger, Diane Normandin, and John E. Macor [Full Article - PDF]

5044-5049

Synthesis and Evaluation of Isothiocyanate-Containing Derivatives of the -Opioid Receptor Antagonist Tyr-Tic-Phe-Phe (TIPP) as Potential Affinity Labels for -Opioid Receptors Dean Y. Maeda, Fred Berman, Thomas F. Murray, and Jane V. Aldrich [Full Article - PDF]

5050-5054

Extended TIP(P) Analogues as Precursors for Labeled -Opioid Receptor Ligands Vivek Kumar, Thomas F. Murray, and Jane V. Aldrich [Full Article - PDF]

BOOK REVIEWS

5055-5055

Annual Reports in Medicinal Chemistry. Volume 35 Editor-in-Chief, Annette Doherty. Academic Press, San Diego, CA. 2000. xi + 425 pp. 17.5 × 25.5 cm. ISBN 0-12-040535-0. $85.00. Staff [Full Article - PDF]

5055-5055

Analytical Techniques in Combinatorial Chemistry Edited by Michael Swartz. Marcel Dekker, New York. 2000. xii + 301 pp. 15.5 × 23.5 cm. ISBN 0-8247-1939-5. $150.00. Robert G. Gentles [Full Article - PDF]

5055-5056

Topological Indices and Related Descriptors in QSAR and QSPR Edited by James Devillers and Alexandru T. Balaban. Gordon and Breach Science Publishers, Amsterdam, The Netherlands. 1999. x + 811 pp. 15.5 × 23.5 cm. ISBN 90-5699-239-2. $198.00. William J. Dunn III [Full Article - PDF]

ADDITIONS AND CORRECTIONS

5057-5057

Synthesis and SAR of New 5-Phenyl-3-ureido-1,5-benzodiazepines as Cholecystokinin-B Receptor Antagonists. Antonella Ursini, Anna M. Capelli, Robin A. E. Carr, Paolo Cassarà, Mauro Corsi, Ornella Curcuruto, Giovanni Curotto, Michele Dal Cin, Silvia Davalli, Daniele Donati, Aldo Feriani, Harry Finch, Gabriella Finizia, Giovanni Gaviraghi, Marc Marien, Giorgio Pentassuglia, Stefano Polinelli, Emiliangelo Ratti, Aldo Reggiani, Giorgio Tarzia, Giovanna Tedesco, Maria E. Tranquillini, David G. Trist, and Frank T. M. Van Amsterdam: [Full Article - PDF]

5057-5057

Principles of Process Research and Chemical Development in the Pharmaceutical Industry. Edited by David J. Ager. Marcel Dekker, Inc., New York. 1999. x + 382 pp. 16 × 24 cm. ISBN 0-8247-1058-4. $165.00. Pat N. Confalone: [Full Article - PDF]