Journal of Medicinal Chemistry
Volume 40, Issue 23 (November 7, 1997)
Copyright © 1997 American Chemical Society

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3707-3711

Synthesis of 5,6-Dihydro-4-hydroxy-2- pyrones as HIV-1 Protease Inhibitors: The Profound Effect of Polarity on Antiviral Activity Susan E. Hagen, J. V. N. Vara Prasad, Frederick E. Boyer, John M. Domagala, Edmund L. Ellsworth, Christopher Gajda, Harriet W. Hamilton, Larry J. Markoski, Bruce A. Steinbaugh, Bradley D. Tait, Elizabeth A. Lunney, Peter J. Tummino, Donna Ferguson, Donald Hupe, Carolyn Nouhan, Stephen J. Gracheck, James M. Saunders, and Steven VanderRoest [Full Article - PDF]

3712-3714

Potent and Selective 1,2,3-Trisubstituted Indole NPY Y-1 Antagonists Philip A. Hipskind, Karen L. Lobb, James A. Nixon, Thomas C. Britton, Robert F. Bruns, John Catlow, Donna K. Dieckman-McGinty, Susan L. Gackenheimer, Bruce D. Gitter, Smriti Iyengar, Douglas A. Schober, Rosa M. A. Simmons, Steve Swanson, Hamideh Zarrinmayeh, Dennis M. Zimmerman, and Donald R. Gehlert [Full Article - PDF]

3715-3718

Synthesis and Antimalarial Activity in Vitro and in Vivo of a New Ferrocene-Chloroquine Analogue Christophe Biot, Guillaume Glorian, Lucien A. Maciejewski, and Jacques S. Brocard , Olivier Domarle, Georgette Blampain, Pascal Millet, and Alain J. Georges , Huguette Abessolo and Daniel Dive , Jacques Lebibi [Full Article - PDF]

3719-3725

Design, Synthesis, and Cocrystal Structure of a Nonpeptide Src SH2 Domain Ligand Mark S. Plummer, Debra R. Holland, Aurash Shahripour, Elizabeth A. Lunney, James H. Fergus, James S. Marks, Patrick McConnell, W. Thomas Mueller, and Tomi K. Sawyer [Full Article - PDF]

3726-3733

Discovery of a Novel, Selective, and Orally Bioavailable Class of Thrombin Inhibitors Incorporating Aminopyridyl Moieties at the P1 Position Dong-Mei Feng, Stephen J. Gardell, S. Dale Lewis, Mark G. Bock, Zhongguo Chen, Roger M. Freidinger, Adel M. Naylor-Olsen, Harri G. Ramjit, Richard Woltmann, Elizabeth P. Baskin, Joseph J. Lynch, Robert Lucas, Jules A. Shafer, Kimberley B. Dancheck, I-Wu Chen, Shi-Shan Mao, Julie A. Krueger, Timothy R. Hare, Anne M. Mulichak, and Joseph P. Vacca [Full Article - PDF]

3734-3738

1,4-Disubstituted Anthracene Antitumor Agents Bhashyam S. Iyengar, Robert T. Dorr, David S. Alberts, Anikó M. Sólyom, Mary Krutzsch, and William A. Remers [Full Article - PDF]

3739-3748

Betidamino Acid Scan of the GnRH Antagonist Acyline Guangcheng Jiang, Charleen Miller, Steven C. Koerber, John Porter, A. Grey Craig, Sheela Bhattacharjee, Patricia Kraft, Thomas P. Burris, Carolyn A. Campen, Catherine L. Rivier, and Jean E. Rivier [Full Article - PDF]

3749-3755

1-[(-Aminoalkyl)amino]-4-[N-(-aminoalkyl)carbamoyl]-9-oxo-9,10-dihydro- acridines as Intercalating Cytotoxic Agents: Synthesis, DNA Binding, and Biological Evaluation Ippolito Antonini, Paolo Polucci, Terence C. Jenkins, Lloyd R. Kelland, Ernesto Menta, Nicoletta Pescalli, Barbara Stefanska, Jan Mazerski, and Sante Martelli [Full Article - PDF]

3756-3764

Synthesis and Biological Evaluation of 4-(Hydroxyalkyl)estradiols and Related Compounds Carl J. Lovely, Abhijit S. Bhat, Holly D. Coughenour, Nancy E. Gilbert, and Robert W. Brueggemeier [Full Article - PDF]

3765-3772

N6-Cyclopentyl-3'-substituted-xylofuranosyladenosines: A New Class of Non-Xanthine Adenosine A1 Receptor Antagonists Serge Van Calenbergh, Jacobien K. von Frijtag Drabbe Künzel, Norbert M. Blaton, Oswald M. Peeters, Jef Rozenski, Arthur Van Aerschot, Andre De Bruyn, Denis De Keukeleire, Adriaan P. IJzerman, and Piet Herdewijn [Full Article - PDF]

3773-3780

Simple Analogues of Anthralin: Unusual Specificity of Structure and Antiproliferative Activity Klaus Müller, Helge Prinz, Ingo Gawlik, Klaus Ziereis, and Hsu-Shan Huang [Full Article - PDF]

3781-3792

4-Hydroxy-5,6-dihydropyrones. 2. Potent Non-Peptide Inhibitors of HIV Protease Bradley D. Tait, Susan Hagen, John Domagala, Edmund L. Ellsworth, Christopher Gajda, Harriet W. Hamilton, J. V. N. Vara Prasad, Donna Ferguson, Neil Graham, Donald Hupe, Carolyn Nouhan, Peter J. Tummino, Christine Humblet, Elizabeth A. Lunney, Alexander Pavlovsky, John Rubin, Stephen J. Gracheck, Eric T. Baldwin, T. N. Bhat, John W. Erickson, Sergei V. Gulnik, and Beishan Liu [Full Article - PDF]

3793-3803

Design and Synthesis of Imidazoline Derivatives Active on Glucose Homeostasis in a Rat Model of Type II Diabetes. 1. Synthesis and Biological Activities of N-Benzyl-N '-(arylalkyl)-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines Frédéric Rondu, Gaëlle Le Bihan, Xuan Wang, Aazdine Lamouri, Estera Touboul, Georges Dive, Tounès Bellahsene, Bruno Pfeiffer, Pierre Renard, Béatrice Guardiola-Lemaitre, Dominique Manechez, Luc Penicaud, Alain Ktorza, and Jean-Jacques Godfroid [Full Article - PDF]

3804-3819

Antimuscarinic 3-(2-Furanyl)quinuclidin-2-ene Derivatives: Synthesis and Structure-Activity Relationships Gary Johansson, Staffan Sundquist, Gunnar Nordvall, Björn M. Nilsson, Magnus Brisander, Lisbeth Nilvebrant, and Uli Hacksell [Full Article - PDF]

3820-3828

Synthesis and Biological Activity of a Series of Potent Fluoromethyl Ketone Inhibitors of Recombinant Human Calpain I Sankar Chatterjee, Mark A. Ator, Donna Bozyczko-Coyne, Kurt Josef, Gregory Wells, Rabindranath Tripathy, Mohamed Iqbal, Ron Bihovsky, Shobha E. Senadhi, Satish Mallya, Teresa M. O'Kane, Beth Ann McKenna, Robert Siman, and John P. Mallamo [Full Article - PDF]

3829-3835

Synthesis and Evaluation of (S)-4-(3-(2'-[11C]Isopropylamino)-2-hydroxypropoxy)-2H-benzimidazol-2-one ((S)-[11C]CGP 12388) and (S)-4-(3-((1'-[18F]Fluoroisopropyl)amino)-2-hydroxypropoxy)-2H-benzimidazol-2-one ((S)-[18F]Fluoro-CGP 12388) for Visualization of -Adrenoceptors with Positron Emission Tomography Philip H. Elsinga, Aren van Waarde, Knut A. Jaeggi, Gérard Schreiber, Marco Heldoorn, and Willem Vaalburg [Full Article - PDF]

3836-3841

Synthesis and Structure-Activity Profiles of A-Homoestranes, the Estratropones Thomas A. Miller, Amanda L. Bulman, Charles D. Thompson, Michael E. Garst, and Timothy L. Macdonald [Full Article - PDF]

3842-3850

Design, Synthesis, and Biochemical Evaluation of Phosphonate and Phosphonamidate Analogs of Glutathionylspermidine as Inhibitors of Glutathionylspermidine Synthetase/Amidase from Escherichia coli Shoujun Chen, Chun-Hung Lin, David S. Kwon, Christopher T. Walsh, and James K. Coward [Full Article - PDF]

3851-3857

Retinoic Acid Conjugates as Potential Antitumor Agents: Synthesis and Biological Activity of Conjugates with Ara-A, Ara-C, 3(2H)-Furanone, and Aniline Mustard Moieties Stefano Manfredini, Daniele Simoni, Roberto Ferroni, Rita Bazzanini, Silvia Vertuani, Sigrid Hatse, Jan Balzarini, and Erik De Clercq [Full Article - PDF]

3858-3859

Combinatorial Chemistry. Synthesis and Application Edited by Stephen R. Wilson and Anthony W. Czarnik. John Wiley & Sons. 1997. ix + 269 pp. 16 × 24 cm. ISBN 0-471-12687-X. $69.95. Michael R. Pavia [Full Article - PDF]

3859-3859

The Chemistry of Mind-Altering Drugs. History, Pharmacology, and Cultural Context By Daniel M. Perrine. American Chemical Society, Washington, D.C. 1996. x + 480 pp. 17.5 × 25 cm. ISBN 0-8412-3253-9. $39.95. David E. Nichols [Full Article - PDF]

3859-3860

Studies in Medicinal Chemistry. Volume 2. Biological Inhibitors Edited by M. Iqbal Choudhary. Harwood Academic Publishers GmbH, Amsterdam. 1996. xiv + 378 pp. 17.5 × 25.3 cm. ISBN 3-7186-5879-8. $150.00. Joseph Weinstock [Full Article - PDF]

3860-3860

Burgers' Medicinal Chemistry and Drug Discovery. Volume 4 Edited by M. E. Wolff. John Wiley & Sons, New York. 1997. viii + 656 pp. 18.5 × 26 cm. ISBN 0-471-57559-3. $225.00. Lemont B. Kier [Full Article - PDF]