Journal of Medicinal Chemistry
Volume 40, Issue 16 (August 1, 1997)
Copyright © 1997 American Chemical Society

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2435-2439

Synthesis and Biology of a 7-Nitro-2,1,3-benzoxadiazol-4-yl Derivative of 2-Phenylindole-3-acetamide: A Fluorescent Probe for the Peripheral-Type Benzodiazepine Receptor Alan P. Kozikowski, Maria Kotoula, Dawei Ma, Noureddine Boujrad, Werner Tückmantel, and Vassilios Papadopoulos [Full Article - PDF]

2440-2444

An Orally Bioavailable Pyrrolinone Inhibitor of HIV-1 Protease: Computational Analysis and X-ray Crystal Structure of the Enzyme Complex Amos B. Smith, III, Ralph Hirschmann, Alexander Pasternak, Wenquing Yao, and Paul A. Sprengeler , M. Katharine Holloway, Lawrence C. Kuo, Zhongguo Chen, Paul L. Darke, and William A. Schleif [Full Article - PDF]

2445-2451

Identification of Highly Potent Retinoic Acid Receptor -Selective Antagonists Min Teng, Tien T. Duong, Alan T. Johnson, Elliott S. Klein, Liming Wang, Berket Khalifa, and Roshantha A. S. Chandraratna [Full Article - PDF]

2452-2461

Doxoform and Daunoform: Anthracycline-Formaldehyde Conjugates Toxic to Resistant Tumor Cells David J. Fenick, Dylan J. Taatjes, and Tad H. Koch [Full Article - PDF]

2462-2465

Anti-Helicobacter pylori Agents. 1. 2-(Alkylguanidino)-4-furylthiazoles and Related Compounds Yousuke Katsura, Tetsuo Tomishi, Yoshikazu Inoue, Kazuo Sakane, Yoshimi Matsumoto, Hirohumi Ishikawa, and Hisashi Takasugi [Full Article - PDF]

2466-2473

Selective Inhibitors of Monoamine Oxidase. 4. SAR of Tricyclic N-Methylcarboxamides and Congeners Binding at the Tricyclics' Hydrophilic Binding Site Morton Harfenist, Diane M. Joseph, Sharon C. Spence, Daniel P. C. Mcgee, Mark D. Reeves, and Helen L. White [Full Article - PDF]

2474-2481

Synthesis and Ligand Binding Studies of 4'-Iodobenzoyl Esters of Tropanes and Piperidines at the Dopamine Transporter Satendra Singh, Garo P. Basmadjian, Kwasi S. Avor, Buddy Pouw, and Thomas W. Seale [Full Article - PDF]

2482-2490

Synthesis and in Vitro Activity of Long-Chain 5'-O-[(Alkoxycarbonyl)phosphinyl]-3'-azido-3'-deoxythymidines against Wild-Type and AZT- and Foscarnet-Resistant Strains of HIV-1 Andre Rosowsky, Hongning Fu, Niranjan Pai, John Mellors, Douglas D. Richman, and Karl Y. Hostetler [Full Article - PDF]

2491-2501

5-(Piperidin-2-yl)- and 5-(Homopiperidin-2-yl)-1,4-benzodiazepines: High-Affinity, Basic Ligands for the Cholecystokinin-B Receptor José L. Castro, Howard B. Broughton, Michael G. N. Russell, Denise Rathbone, Alan P. Watt, Richard G. Ball, Kerry L. Chapman, Smita Patel, Alison J. Smith, George R. Marshall, and Victor G. Matassa [Full Article - PDF]

2502-2524

Protein Structure-Based Design, Synthesis, and Biological Evaluation of 5-Thia-2,6-diamino-4(3H)-oxopyrimidines: Potent Inhibitors of Glycinamide Ribonucleotide Transformylase with Potent Cell Growth Inhibition Michael D. Varney, Cindy L. Palmer, William H. Romines III, Theodore Boritzki, Stephen A. Margosiak, Robert Almassy, Cheryl A. Janson, Charlotte Bartlett, Eleanor J. Howland, and Rosanne Ferre [Full Article - PDF]

2525-2532

Discovery of CGS 27023A, a Non-Peptidic, Potent, and Orally Active Stromelysin Inhibitor That Blocks Cartilage Degradation in Rabbits Lawrence J. MacPherson*, Erol K. Bayburt, Michael P. Capparelli, Brian J. Carroll, Robert Goldstein, Michael R. Justice, Lijuan Zhu, Shou-ih Hu, Richard A. Melton, Lynn Fryer, Ron L. Goldberg, John R. Doughty, Salvatore Spirito, Vincent Blancuzzi, Doug Wilson, Elizabeth M. O'Byrne, Vishwas Ganu, and David T. Parker* [Full Article - PDF]

2533-2538

Synthesis of Nonhydrolyzable Analogues of Thiazole-4-carboxamide and Benzamide Adenine Dinucleotide Containing Fluorine Atom at the C2' of Adenine Nucleoside: Induction of K562 Differentiation and Inosine Monophosphate Dehydrogenase Inhibitory Activity Krystyna Lesiak, Kyoichi A. Watanabe, Alokes Majumdar, Michael Seidman, Kristen Vanderveen, Barry M. Goldstein, and Krzysztof W. Pankiewicz [Full Article - PDF]

2539-2546

Novel 99mTc Aminobisthiolato/Monothiolato "3 + 1" Mixed Ligand Complexes: Structure-Activity Relationships and Preliminary in Vivo Validation as Brain Blood Flow Imaging Agents Ioannis C. Pirmettis, Minas S. Papadopoulos, and Efstratios Chiotellis [Full Article - PDF]

2547-2554

Steroidal Glycoside Cholesterol Absorption Inhibitors Michael P. DeNinno, Peter A. McCarthy, Kimberly C. Duplantier, Cynthia Eller, John B. Etienne, Michael P. Zawistoski, Faan Wen Bangerter, Charles E. Chandler, Lee A. Morehouse, Eliot D. Sugarman, Robert W. Wilkins, Heidi A. Woody, and Lawrence M. Zaccaro [Full Article - PDF]

2555-2562

The Role of Phenylalanine at Position 6 in Glucagon's Mechanism of Biological Action: Multiple Replacement Analogues of Glucagon Bassem Y. Azizeh, Jung-Mo Ahn, Rael Caspari, Mark D. Shenderovich, Dev Trivedi, and Victor J. Hruby [Full Article - PDF]

2563-2570

The Chemistry of Pseudomonic Acid. 18. Heterocyclic Replacement of the ,-Unsaturated Ester: Synthesis, Molecular Modeling, and Antibacterial Activity Pamela Brown, Desmond J. Best, Nigel J. P. Broom, Robert Cassels, Peter J. O'Hanlon, Timothy J. Mitchell, Neal F. Osborne, and Jennifer M. Wilson [Full Article - PDF]

2571-2578

H3-Receptor Antagonists: Synthesis and Structure-Activity Relationships of Para- and Meta-Substituted 4(5)-Phenyl-2-[[2-[4(5)-imidazolyl]ethyl]thio]imidazoles Marco Mor, Fabrizio Bordi, Claudia Silva, Silvia Rivara, Patrizia Crivori, Pier Vincenzo Plazzi, Vigilio Ballabeni, Antonio Caretta, Elisabetta Barocelli, Mariannina Impicciatore, Pierre-Alain Carrupt, and Bernard Testa [Full Article - PDF]

2579-2587

Helix-Inducing -Aminoisobutyric Acid in Opioid Mimetic Deltorphin C Analogues Sharon D. Bryant, Remo Guerrini, Severo Salvadori, Clementina Bianchi, Roberto Tomatis, Martti Attila, and Lawrence H. Lazarus [Full Article - PDF]

2588-2595

Mutagenesis Reveals Structure-Activity Parallels between Human A2A Adenosine Receptors and Biogenic Amine G Protein-Coupled Receptors Qiaoling Jiang, Brian X. Lee, Marc Glashofer, A. Michiel van Rhee, and Kenneth A. Jacobson [Full Article - PDF]

2596-2608

Structure-Activity Relationships of 4-(Phenylethynyl)-6-phenyl-1,4- dihydropyridines as Highly Selective A3 Adenosine Receptor Antagonists Ji-long Jiang, A. Michiel van Rhee, Louis Chang, Abraham Patchornik, Xiao-duo Ji, Patricia Evans, Neli Melman, and Kenneth A. Jacobson [Full Article - PDF]

2609-2625

Design and Synthesis of Novel Imidazole-Substituted Dipeptide Amides as Potent and Selective Inhibitors of Candida albicans MyristoylCoA:Protein N-Myristoyltransferase and Identification of Related Tripeptide Inhibitors with Mechanism-Based Antifungal Activity Balekudru Devadas, Sandra K. Freeman, Mark E. Zupec, Hwang-Fun Lu, Srinivasan R. Nagarajan, Nandini S. Kishore, Jennifer K. Lodge, David W. Kuneman, Charles A. McWherter, Dutt V. Vinjamoori, Daniel P. Getman, Jeffrey I. Gordon, and James A. Sikorski [Full Article - PDF]

2626-2633

Synthesis and Antimetastatic Activity of L-Iduronic Acid-Type 1-N-Iminosugars Yoshio Nishimura, Takahiko Satoh, Hayamitsu Adachi, Shinichi Kondo, Tomio Takeuchi, Masayuki Azetaka, Harumi Fukuyasu, and Yumiko Iizuka [Full Article - PDF]

2634-2642

Structure-Activity Relationships for the Antileishmanial and Antitrypanosomal Activities of 1'-Substituted 9-Anilinoacridines Swarna A. Gamage, David P. Figgitt, Stanley J. Wojcik, Raymond K. Ralph, Adriana Ransijn, Jacques Mauel, Vanessa Yardley, Diane Snowdon, Simon L. Croft, and William A. Denny [Full Article - PDF]

2643-2652

A Novel Radioiodination Reagent for Protein Radiopharmaceuticals with L-Lysine as a Plasma-Stable Metabolizable Linkage To Liberate m-Iodohippuric Acid after Lysosomal Proteolysis Kouji Wakisaka, Yasushi Arano, Takashi Uezono, Hiromichi Akizawa, Masahiro Ono, Keiichi Kawai, Yoshiro Ohomomo, Morio Nakayama, and Hideo Saji [Full Article - PDF]

2653-2656

Synthesis and Structure-Activity Relationships of a New Model of Arylpiperazines. 3. 2-[-(4-Arylpiperazin-1-yl)alkyl]perhydropyrrolo- [1,2-c]imidazoles and -perhydroimidazo[1,5-a]pyridines: Study of the Influence of the Terminal Amide Fragment on 5-HT1A Affinity/Selectivity María L. López-Rodríguez, M. José Morcillo, Esther Fernández, Esther Porras, Marta Murcia, Antonio M. Sanz, and Luis Orensanz [Full Article - PDF]

2657-2657

Tutorials for the Biomedical Sciences. Animations, Simulations, and Calculations using Mathematica Edited by Charles Pidgeon. VCH Publishers Inc., New York. 1996. xxvii + 300 pp. 21.5 × 28 cm. ISBN 1-56081-928-6. $79.95.Advanced Tutorials for the Biomedical Sciences. Animations, Simulations, and Calculations using Mathematica Edited by Charles Pidgeon. VCH Publishers Inc., New York. 1996. xxvii + 275 pp. 21.5 × 28 cm. ISBN 1-56081-950-2. $79.95. Donald J. Abraham [Full Article - PDF]

2657-2658

Goodman & Gilman's The Pharmacological Basis of Therapeutics Edited by Joel G. Hardman, Lee E. Limbird, Perry B. Molinoff, and Raymond W. Ruddon. McGraw-Hill, New York. 1996. xxi + 1905 pp. 21 × 26 cm. ISBN 0-07-026266-7. $89.00. S. J. Enna [Full Article - PDF]

2658-2658

Textbook of Biochemistry With Clinical Correlations. Fourth Edition Edited by Thomas M. Devlin. Wiley-Liss, Inc., New York. 1997. xxvii + 1186 pp. 22.5 × 28.5 cm. ISBN 0-471-15451-2. $84.95. Staff [Full Article - PDF]

2658-2659

Dictionary of Plant Toxins Edited by Jeffrey B. Harborne and Herbert Baxter; Associate Editor Gerard P. Moss. John Wiley & Sons, Chichester. 1996. xv + 523 pp. 22 × 28.5 cm. ISBN 0-471-95107-2. $195.00. Maurice Shamma [Full Article - PDF]

2659-2659

Annual Review of Pharmacology and Toxicology. Volume 37, 1997 Edited by Arthur K. Cho. Annual Reviews, Inc., Palo Alto, CA. 1997. x + 571 pp. 16 × 23 cm. ISBN 0-8243-0437-3. $60.00. Staff [Full Article - PDF]

2659-2659

Books of Interest [Full Article - PDF]

2660-2660

2-[2'-(Dimethylamino)ethyl]-1,2-dihydro-3H-dibenz[de,h]isoquinoline-1,3-diones with Substituents at Positions 4, 8, 9, 10, and 11. Synthesis, Antitumor Activity, and Quantitative Structure-Activity Relationships Salah M. Sami, Robert T. Dorr, David S. Alberts, Anikó M. Sólyom, and William A. Remers [Full Article - PDF]