Journal of Medicinal Chemistry
Volume 39, Issue 23 (November 8, 1996)
Copyright © 1996 American Chemical Society

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4527-4530

Potent and Selective Thrombin Inhibitors Incorporating the Constrained Arginine Mimic L-3-Piperidyl(N-guanidino)alanine at P1 Odile E. Levy, J. Edward Semple, Michael L. Lim, John Reiner, William E. Rote, Erin Dempsey, Brigitte M. Richard, Erli Zhang, Al Tulinsky, William C. Ripka, and Ruth F. Nutt [Full Article - PDF]

4531-4536

Design, Synthesis, and Evolution of a Novel, Selective, and Orally Bioavailable Class of Thrombin Inhibitors: P1-Argininal Derivatives Incorporating P3-P4 Lactam Sulfonamide Moieties J. Edward Semple, David C. Rowley, Terence K. Brunck, Theresa Ha-Uong, Nathaniel K. Minami, Timothy D. Owens, Susan Y. Tamura, Erick A. Goldman, Daniel V. Siev, Robert J. Ardecky, Stephen H. Carpenter, Yu Ge, Brigitte M. Richard, Thomas G. Nolan, Kjell Håkanson, Al Tulinsky, Ruth F. Nutt, and William C. Ripka [Full Article - PDF]

4537-4539

Synthesis of Novel trans-4-(Substituted-benzamido)-3,4-dihydro-2H-benzo[b]pyran-3-ol Derivatives as Potential Anticonvulsant Agents with a Distinctive Binding Profile Wai N. Chan, John M. Evans, Michael S. Hadley, Hugh J. Herdon, Jeffrey C. Jerman, Helen K. A. Morgan, Tania O. Stean, Mervyn Thompson, Neil Upton, and Antonio K. Vong [Full Article - PDF]

4540-4546

High-Resolution Crystal Structures of Human Cyclin-Dependent Kinase 2 with and without ATP: Bound Waters and Natural Ligand as Guides for Inhibitor Design Ursula Schulze-Gahmen, Hendrik L. De Bondt, and Sung-Hou Kim [Full Article - PDF]

4547-4553

Studies on Selectin Blocker. 3. Investigation of the Carbohydrate Ligand Sialyl Lewis X Recognition Site of P-Selectin Yasuyuki Hiramatsu, Hideki Tsujishita, and Hirosato Kondo [Full Article - PDF]

4554-4562

Targeting the Minor Groove of DNA: Crystal Structures of Two Complexes between Furan Derivatives of Berenil and the DNA Dodecamer d(CGCGAATTCGCG)2 John O. Trent, George R. Clark, Arvind Kumar, W. David Wilson, David W. Boykin, James Edwin Hall, Richard R. Tidwell, Byron L. Blagburn, and Stephen Neidle [Full Article - PDF]

4563-4568

2-Amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines as Nonclassical Antifolate Inhibitors of Thymidylate Synthase1a,b Aleem Gangjee, Farahnaz Mavandadi, Roy L. Kisliuk, John J. McGuire, and Sherry F. Queener [Full Article - PDF]

4569-4575

Synthesis and Biological Activity of Aromatic Amino Acid Phosphoramidates of 5-Fluoro-2'-deoxyuridine and 1--Arabinofuranosylcytosine: Evidence of Phosphoramidase Activity Timothy W. Abraham, Thomas I. Kalman, Edward J. McIntee, and Carston R. Wagner [Full Article - PDF]

4576-4582

Synthesis, Biological Evaluation, Calcium Channel Antagonist Activity, and Anticonvulsant Activity of Felodipine Coupled to a Dihydropyridine-Pyridinium Salt Redox Chemical Delivery System Sai-hay Yiu and Edward E. Knaus [Full Article - PDF]

4583-4591

Non-Peptide Glycoprotein IIb/IIIa Antagonists. 11. Design and in Vivo Evaluation of 3,4-Dihydro-1(1H)-isoquinolinone-Based Antagonists and Ethyl Ester Prodrugs John H. Hutchinson, Jacquelynn J. Cook, Karen M. Brashear, Michael J. Breslin, Joan D. Glass, Robert J. Gould, Wasyl Halczenko, Marie A. Holahan, Robert J. Lynch, Gary R. Sitko, Maria T. Stranieri, and George D. Hartman [Full Article - PDF]

4592-4601

N-Aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropanamides: KATP Potassium Channel Openers. Modifications on the Western Region Cyrus J. Ohnmacht, Keith Russell, James R. Empfield, Cathy A. Frank, Keith H. Gibson, Daniel R. Mayhugh, Frances M. McLaren, Howard S. Shapiro, Frederick J. Brown, Diane A. Trainor, Christopher Ceccarelli, Margaret M. Lin, Brian B. Masek, Janet M. Forst, Robert J. Harris, James M. Hulsizer, Joseph J. Lewis, Stuart M. Silverman, Reed W. Smith, Paul J. Warwick, Sen T. Kau, Alexa L. Chun, Thomas L. Grant, Burton B. Howe, Jack H. Li, Shephali Trivedi, Tracy J. Halterman, Christopher Yochim, Martin C. Dyroff, M. Kirkland, and Kathleen L. Neilson [Full Article - PDF]

4602-4607

Synthesis and Biological Profile of the Enantiomers of [4-(4-Amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin-1-yl]furan- 2-ylmethanone (Cyclazosin), a Potent Competitive 1B-Adrenoceptor Antagonist Dario Giardinà, Mauro Crucianelli, Roberta Romanelli, Amedeo Leonardi, Elena Poggesi, and Carlo Melchiorre [Full Article - PDF]

4608-4621

Synthesis, Structure-Activity Relationships, and Pharmacokinetic Properties of Dihydroorotate Dehydrogenase Inhibitors: 2-Cyano-3-cyclopropyl-3-hydroxy- N-[3'-methyl-4'-(trifluoromethyl)phenyl]propenamide and Related Compounds Elizabeth A. Kuo, Philip T. Hambleton, David P. Kay, Phillip L. Evans, Saroop S. Matharu, Edward Little, Neil McDowall, C. Beth Jones, Charles J. R. Hedgecock, Christopher M. Yea, A. W. Edith Chan, Peter W. Hairsine, Ian R. Ager, W. Roger Tully, Richard A. Williamson, and Robert Westwood [Full Article - PDF]

4622-4629

Molecular Electronic Properties of a Series of 4-Quinolinecarbinolamines Define Antimalarial Activity Profile Apurba K. Bhattacharjee and Jean M. Karle [Full Article - PDF]

4630-4642

Structure-Based Design of HIV Protease Inhibitors: 5,6-Dihydro-4-hydroxy-2-pyrones as Effective, Nonpeptidic Inhibitors Suvit Thaisrivongs, Donna L. Romero, Ruben A. Tommasi, Musiri N. Janakiraman, Joseph W. Strohbach, Steve R. Turner, Carolyn Biles, Raymond R. Morge, Paul D. Johnson, Paul A. Aristoff, Paul K. Tomich, Janet C. Lynn, Miao-Miao Horng, Kong-Teck Chong, Roger R. Hinshaw, W. Jeffrey Howe, Barry C. Finzel, and Keith D. Watenpaugh [Full Article - PDF]

4643-4653

Analogs of 3-Hydroxy-1H-1-benzazepine-2,5-dione: Structure-Activity Relationship at N-Methyl-D-aspartate Receptor Glycine Sites Anthony P. Guzikowski, Sui Xiong Cai, Stephen A. Espitia, Jon E. Hawkinson, James E. Huettner, Daniel F. Nogales, Minhtam Tran, Richard M. Woodward, Eckard Weber, and John F. W. Keana [Full Article - PDF]

4654-4666

High-Affinity -Aminobutyric Acid A/Benzodiazepine Ligands: Synthesis and Structure-Activity Relationship Studies of a New Series of Tetracyclic Imidazoquinoxalines John W. Mickelson, E. Jon Jacobsen, Donald B. Carter, Haesook K. Im, Wha Bin Im, Peggy J. K. D. Schreur, Vimala H. Sethy, Andy H. Tang, James E. McGee, and James D. Petke [Full Article - PDF]

4667-4675

6-Phenyl-1,4-dihydropyridine Derivatives as Potent and Selective A3 Adenosine Receptor Antagonists Ji-long Jiang, A. Michiel van Rhee, Neli Melman, Xiao-duo Ji, and Kenneth A. Jacobson [Full Article - PDF]

4676-4681

In Vitro and in Vivo Evaluation of 6-Azido-2',3'-dideoxy-2'-fluoro--D-arabinofuranosylpurine and N6-Methyl-2',3'-dideoxy-2'-fluoro--D-arabinofuranosyladenine as Prodrugs of the Anti-HIV Nucleosides 2'-F-ara-ddA and 2'-F-ara-ddI Tanya Koudriakova, Konstantine K. Manouilov, Kirupa Shanmuganathan, Lakshmi P. Kotra, F. Douglas Boudinot, Erica Cretton-Scott, Jean-Pierre Sommadossi, Raymond F. Schinazi, and Chung K. Chu [Full Article - PDF]

4682-4686

Structure-Activity Relationships of 4-Hydroxy-3-nitroquinolin-2(1H)-ones as Novel Antagonists at the Glycine Site of N-Methyl-D-aspartate Receptors Sui Xiong Cai, Zhang-Lin Zhou, Jin-Cheng Huang, Edward R. Whittemore, Zizi O. Egbuwoku, Jon E. Hawkinson, Richard M. Woodward, Eckard Weber, and John F. W. Keana [Full Article - PDF]

4687-4687

Biotechnology Intelligence Unit. Structure-Property Correlations in Drug Development Edited by Han van de Waterbeemd. Academic Press, Inc., San Diego, CA. Academic Press Ltd., London, United Kingdom. R. G. Landes Co., Georgetown, TX. 1996. 210 pp. 18.5 × 26 cm. ISBN 0-12-711650-8. $69.95. Donald T. Witiak [Full Article - PDF]

4687-4687

The Practice of Medicinal Chemistry Edited by Camille G. Wermuth. Academic Press, London. 1996. xvii + 968 pp. 17 × 25 cm. ISBN 0-12-744640-0. $89.00. Manfred E. Wolff [Full Article - PDF]

4687-4688

Bioorganic Chemistry. A Chemical Approach to Enzyme Action. Third Edition Hermann Dugas. Springer-Verlag, New York. 1996. xvii + 700 pp. 16 × 24 cm. ISBN 0-387-94494-X. $49.95. Joseph G. Cannon [Full Article - PDF]

4688-4688

Books of Interest [Full Article - PDF]