Journal of Medicinal Chemistry
Volume 41, Issue 15 (July 16, 1998)
Copyright © 1998 American Chemical Society

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COMMUNICATIONS TO THE EDITOR

2663-2666

D-Amino Acid Containing, High-Affinity Inhibitors of Recombinant Human Calpain I Sankar Chatterjee, Zi-Qiang Gu, Derek Dunn, Ming Tao, Kurt Josef, Rabindranath Tripathy, Ron Bihovsky, Shobha E. Senadhi, Teresa M. O'Kane, Beth Ann McKenna, Satish Mallya, Mark A. Ator, Donna Bozyczko-Coyne, Robert Siman, and John P. Mallamo [Full Article - PDF]

2667-2670

Enhancement of Oral Absorption in Selective 5-HT1D Receptor Agonists: Fluorinated 3-[3-(Piperidin-1-yl)propyl]indoles José L. Castro, Ian Collins, Michael G. N. Russell, Alan P. Watt, Bindi Sohal, Denise Rathbone, Margaret S. Beer, and Josephine A. Stanton [Full Article - PDF]

2671-2675

Novel and Specific Respiratory Syncytial Virus Inhibitors That Target Virus Fusion Wei-dong Ding, Boris Mitsner, Girija Krishnamurthy, Ann Aulabaugh, Cynthia D. Hess, Joe Zaccardi, Mark Cutler, Boris Feld, Anna Gazumyan, Yuri Raifeld, Antonia Nikitenko, Stanley A. Lang, Yakov Gluzman, Bryan O'Hara, and George A. Ellestad [Full Article - PDF]

2676-2678

Nucleosides and Nucleotides. 177. 9-(6,7-Dideoxy--D-allo-hept-5- ynofuranosyl)adenine: A Selective and Potent Ligand for P3 Purinoceptor-like Protein Akira Matsuda, Haruyo Kosaki, Yoshiko Saitoh, Yuichi Yoshimura, Noriaki Minakawa, and Hiroyasu Nakata [Full Article - PDF]

ARTICLES

2679-2685

Design, Synthesis, and Biological Activities of Potent and Selective Somatostatin Analogues Incorporating Novel Peptoid Residues Thuy-Anh Tran, Ralph-Heiko Mattern, Michel Afargan, Oved Amitay, Ofer Ziv, Barry A. Morgan, John E. Taylor, Daniel Hoyer, and Murray Goodman [Full Article - PDF]

2686-2692

Conformational Analyses of Somatostatin-Related Cyclic Hexapeptides Containing Peptoid Residues Ralph-Heiko Mattern, Thuy-Anh Tran, and Murray Goodman [Full Article - PDF]

2693-2700

Structure-Function Studies on Positions 17, 18, and 21 Replacement Analogues of Glucagon: The Importance of Charged Residues and Salt Bridges in Glucagon Biological Activity Noel S. Sturm, Ying Lin, Stephen K. Burley, John L. Krstenansky, Jung-Mo Ahn, Bassem Y. Azizeh, Dev Trivedi, and Victor J. Hruby [Full Article - PDF]

2701-2708

Synthesis and in Vitro Efficacy of Transferrin Conjugates of the Anticancer Drug Chlorambucil Ulrich Beyer, Thomas Roth, Peter Schumacher, Gerhard Maier, Anuschka Unold, August W. Frahm, Heinz H. Fiebig, Clemens Unger, and Felix Kratz [Full Article - PDF]

2709-2719

Synthesis and Evaluation of a Series of Novel 2-[(4-Chlorophenoxy)methyl]- benzimidazoles as Selective Neuropeptide Y Y1 Receptor Antagonists Hamideh Zarrinmayeh, Anne M. Nunes, Paul L. Ornstein, Dennis M. Zimmerman, M. Brian Arnold, Douglas A. Schober, Susan L. Gackenheimer, Robert F. Bruns, Philip A. Hipskind, Thomas C. Britton, Buddy E. Cantrell, and Donald R. Gehlert [Full Article - PDF]

2720-2731

Indolequinone Antitumor Agents: Reductive Activation and Elimination from (5-Methoxy-1-methyl-4,7-dioxoindol-3-yl)methyl Derivatives and Hypoxia-Selective Cytotoxicity in Vitro Matthew A. Naylor, Elizabeth Swann, Steven A. Everett, Mohammed Jaffar, John Nolan, Naomi Robertson, Stacey D. Lockyer, Kantilal B. Patel, Madeleine F. Dennis, Michael R. L. Stratford, Peter Wardman, Gerald E. Adams, Christopher J. Moody, and Ian J. Stratford [Full Article - PDF]

2732-2744

Selective Endothelin A Receptor Antagonists. 3. Discovery and Structure-Activity Relationships of a Series of 4-Phenoxybutanoic Acid Derivatives Peter C. Astles, Clive Brealey, Thomas J. Brown, Vincenzo Facchini, Caroline Handscombe, Neil V. Harris, Clive McCarthy, Iain M. McLay, Barry Porter, Alan G. Roach, Carol Sargent, Christopher Smith, and Roger J. A. Walsh [Full Article - PDF]

2745-2753

Selective Endothelin A Receptor Antagonists. 4. Discovery and Structure-Activity Relationships of Stilbene Acid and Alcohol Derivatives Peter C. Astles, Thomas J. Brown, Frank Halley, Caroline M. Handscombe, Neil V. Harris, Clive McCarthy, Iain M. McLay, Peter Lockey, Tahir Majid, Barry Porter, Alan G. Roach, Christopher Smith, and Roger Walsh [Full Article - PDF]

2754-2764

Antihyperglycemic Activities of Cryptolepine Analogues: An Ethnobotanical Lead Structure Isolated from Cryptolepis sanguinolenta Donald E. Bierer, Larisa G. Dubenko, Pingsheng Zhang, Qing Lu, Patricia A. Imbach, Albert W. Garofalo, Puay-Wah Phuan, Diana M. Fort, Joane Litvak, R. Eric Gerber, Barbara Sloan, Jian Luo, Raymond Cooper, and Gerald M. Reaven [Full Article - PDF]

2765-2778

Synthesis and Pharmacological Characterization of Novel 6-Fluorochroman Derivatives as Potential 5-HT1A Receptor Antagonists Tomoyuki Yasunaga, Takenori Kimura, Ryo Naito, Toru Kontani, Fumikazu Wanibuchi, Hiroshi Yamashita, Tamako Nomura, Shin-ichi Tsukamoto, Tokio Yamaguchi, and Toshiyasu Mase [Full Article - PDF]

2779-2785

Preparation, Resolution, and Biological Evaluation of 5-Aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines: Potent, Orally Active, Nonsteroidal Progesterone Receptor Agonists James P. Edwards, Lin Zhi, Charlotte L. F. Pooley, Christopher M. Tegley, Sarah J. West, Ming-Wei Wang, Marco M. Gottardis, Charles Pathirana, William T. Schrader, and Todd K. Jones [Full Article - PDF]

2786-2805

Tripeptide Aldehyde Inhibitors of Human Rhinovirus 3C Protease: Design, Synthesis, Biological Evaluation, and Cocrystal Structure Solution of P1 Glutamine Isosteric Replacements Stephen E. Webber, Koji Okano, Thomas L. Little, Siegfried H. Reich, Yue Xin, Shella A. Fuhrman, David A. Matthews, Robert A. Love, Thomas F. Hendrickson, Amy K. Patick, James W. Meador, III, Rose Ann Ferre, Edward L. Brown, Clifford E. Ford, Susan L. Binford, and Stephen T. Worland [Full Article - PDF]

2806-2818

Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. 1. Michael Acceptor Structure-Activity Studies Peter S. Dragovich, Stephen E. Webber, Robert E. Babine, Shella A. Fuhrman, Amy K. Patick, David A. Matthews, Caroline A. Lee, Siegfried H. Reich, Thomas J. Prins, Joseph T. Marakovits, Ethel S. Littlefield, Ru Zhou, Jayashree Tikhe, Clifford E. Ford, Michael B. Wallace, James W. Meador, III, Rose Ann Ferre, Edward L. Brown, Susan L. Binford, James E. V. Harr, Dorothy M. DeLisle, and Stephen T. Worland [Full Article - PDF]

2819-2834

Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. 2. Peptide Structure-Activity Studies Peter S. Dragovich, Stephen E. Webber, Robert E. Babine, Shella A. Fuhrman, Amy K. Patick, David A. Matthews, Siegfried H. Reich, Joseph T. Marakovits, Thomas J. Prins, Ru Zhou, Jayashree Tikhe, Ethel S. Littlefield, Ted M. Bleckman, Michael B. Wallace, Thomas L. Little, Clifford E. Ford, James W. Meador, III, Rose Ann Ferre, Edward L. Brown, Susan L. Binford, Dorothy M. DeLisle, and Stephen T. Worland [Full Article - PDF]

2835-2845

Derivatives of the Triazoloquinazoline Adenosine Antagonist (CGS 15943) Having High Potency at the Human A2B and A3 Receptor Subtypes Yong-Chul Kim, Maarten de Zwart, Louis Chang, Stefano Moro, Jacobien K. von Frijtag Drabbe Künzel, Neli Melman, Ad P. IJzerman, and Kenneth A. Jacobson [Full Article - PDF]

2846-2857

Styrylquinoline Derivatives: A New Class of Potent HIV-1 Integrase Inhibitors That Block HIV-1 Replication in CEM Cells Khalid Mekouar, Jean-François Mouscadet, Didier Desmaële, Frédéric Subra, Hervé Leh, Delphine Savouré, Christian Auclair, and Jean d'Angelo [Full Article - PDF]

2858-2871

N-Phenylamidines as Selective Inhibitors of Human Neuronal Nitric Oxide Synthase: Structure-Activity Studies and Demonstration of in Vivo Activity Jon L. Collins, Barry G. Shearer, Jeffrey A. Oplinger, Shuliang Lee, Edward P. Garvey, Mark Salter, Claire Duffy, Thimysta C. Burnette, and Eric S. Furfine [Full Article - PDF]

2872-2881

Synthesis, Opioid Receptor Binding, and Bioassay of Naltrindole Analogues Substituted in the Indolic Benzene Moiety Subramaniam Ananthan, Cheryl A. Johnson, Ronald L. Carter, Sarah D. Clayton, Kenner C. Rice, Heng Xu, Peg Davis, Frank Porreca, and Richard B. Rothman [Full Article - PDF]

2882-2891

-Lactam Derivatives as Inhibitors of Human Cytomegalovirus Protease Christiane Yoakim, William W. Ogilvie, Dale R. Cameron, Catherine Chabot, Ingrid Guse, Bruno Haché, Julie Naud, Jeff A. O'Meara, Raymond Plante, and Robert Déziel [Full Article - PDF]

2892-2902

Nucleosides and Nucleotides. 175. Structural Requirements of the Sugar Moiety for the Antitumor Activities of New Nucleoside Antimetabolites, 1-(3-C-Ethynyl--D-ribo-pentofuranosyl)cytosine and -uracil Hideshi Hattori, Eisuke Nozawa, Tomoharu Iino, Yuichi Yoshimura, Satoshi Shuto, Yuji Shimamoto, Makoto Nomura, Masakazu Fukushima, Motohiro Tanaka, Takuma Sasaki, and Akira Matsuda [Full Article - PDF]

2903-2909

Prodrugs of Nitroxyl and Nitrosobenzene as Cascade Latentiated Inhibitors of Aldehyde Dehydrogenase Terry T. Conway, Eugene G. DeMaster, Melinda J. C. Lee, and Herbert T. Nagasawa [Full Article - PDF]

BOOK REVIEWS

2910-2910

Frontiers in Neurobiology 3. Amino Acid Neurotransmission Edited by F. Anne Stephenson and Anthony J. Turner. Portland Press, London. 1998. xiv + 247 pp. 16 × 23.5 cm. ISBN 1-85578-0801. $127.50. S. J. Enna [Full Article - PDF]

2910-2910

The P2 Nucleotide Receptors Edited by John T. Turner, Gary A. Weisman, and Jeffrey S. Fedan. Humana Press, Totowa, NJ. 1997. xi + 440 pp. 16 × 23.5 cm. ISBN 0-89603-425-9. $139.00. Shripad S. Bhagwat [Full Article - PDF]