Journal of Medicinal Chemistry
Volume 42, Issue 15 (July 29, 1999)
Copyright © 1999 American Chemical Society

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PERSPECTIVES

2721-2736

Pharmacotherapies for Treatment of Cocaine Abuse: Preclinical Aspects F. Ivy Carroll, Leonard L. Howell, and Michael J. Kuhar [Full Article - PDF]

COMMUNICATIONS

2737-2740

2-(2-Phenylcyclopropyl)imidazolines: Reversed Enantioselective Interaction at I1 and I2 Imidazoline Receptors Wilma Quaglia, Pascal Bousquet, Maria Pigini, Angelo Carotti, Antonio Carrieri, Monique Dontenwill, Francesco Gentili, Mario Giannella, Francoise Maranca, Alessandro Piergentili, and Livio Brasili [Full Article - PDF]

2741-2746

(R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides Are Orally Active Inhibitors of Pyruvate Dehydrogenase Kinase Thomas D. Aicher, Robert C. Anderson, Gregory R. Bebernitz, Gary M. Coppola, Charles F. Jewell, Douglas C. Knorr, Charles Liu, Donald M. Sperbeck, Leonard J. Brand, Robert J. Strohschein, Jiaping Gao, Christine C. Vinluan, Suraj S. Shetty, Carol Dragland, Emma L. Kaplan, Dominick DelGrande, Amin Islam, Xilin Liu, Robert J. Lozito, Wieslawa M. Maniara, R. Erik Walter, and William R. Mann [Full Article - PDF]

2747-2751

New 4-Aminoquinoline Mannich Base Antimalarials. 1. Effect of an Alkyl Substituent in the 5'-Position of the 4'-Hydroxyanilino Side Chain Kaylene J. Raynes, Paul A. Stocks, Paul M. O'Neill, B. Kevin Park, and Stephen A. Ward [Full Article - PDF]

ARTICLES

2752-2759

Design and Synthesis of Isoxazoline Derivatives as Factor Xa Inhibitors. 1 Mimi L. Quan, Ann Y. Liauw, Christopher D. Ellis, James R. Pruitt, David J. Carini, Lori L. Bostrom, Peggy P. Huang, Kimberly Harrison, Robert M. Knabb, Martin J. Thoolen, Pancras C. Wong, and Ruth R. Wexler [Full Article - PDF]

2760-2773

Design and Synthesis of Isoxazoline Derivatives as Factor Xa Inhibitors. 2 Mimi L. Quan, Christopher D. Ellis, Ann Y. Liauw, Richard S. Alexander, Robert M. Knabb, Gilbert Lam, Matthew R. Wright, Pancras C. Wong, and Ruth R. Wexler [Full Article - PDF]

2774-2797

Conformationally Constrained Butyrophenones with Mixed Dopaminergic (D2) and Serotoninergic (5-HT2A, 5-HT2C) Affinities: Synthesis, Pharmacology, 3D-QSAR, and Molecular Modeling of (Aminoalkyl)benzo- and -thienocycloalkanones as Putative Atypical Antipsychotics Enrique Raviña, Jesús Negreira, José Cid, Christian F. Masaguer, Elizabeth Rosa, M. Emilia Rivas, José A. Fontenla, M. Isabel Loza, Helena Tristán, M. Isabel Cadavid, Ferran Sanz, Estrella Lozoya, Angelo Carotti, and Antonio Carrieri [Full Article - PDF]

2798-2804

32-Indolyl Ether Derivatives of Ascomycin: Three-Dimensional Structures of Complexes with FK506-Binding Protein Joseph W. Becker, Jennifer Rotonda, John G. Cryan, Mary Martin, William H. Parsons, Peter J. Sinclair, Greg Wiederrecht, and Frederick Wong [Full Article - PDF]

2805-2815

Synthesis and Amyloid Binding Properties of Rhenium Complexes: Preliminary Progress Toward a Reagent for SPECT Imaging of Alzheimer's Disease Brain Weiguo Zhen, Hogyu Han, Magdalena Anguiano, Cynthia A. Lemere, Cheon-Gyu Cho, and Peter T. Lansbury, Jr. [Full Article - PDF]

2816-2827

Pharmacophore Models of Group I and Group II Metabotropic Glutamate Receptor Agonists. Analysis of Conformational, Steric, and Topological Parameters Affecting Potency and Selectivity Gabriele Costantino, Antonio Macchiarulo, and Roberto Pellicciari [Full Article - PDF]

2828-2843

Riluzole Series. Synthesis and in Vivo "Antiglutamate" Activity of 6-Substituted-2-benzothiazolamines and 3-Substituted-2-imino-benzothiazolines Patrick Jimonet, François Audiau, Michel Barreau, Jean-Charles Blanchard, Alain Boireau, Yvette Bour, Marie-Annick Coléno, Adam Doble, Gilles Doerflinger, Claudine Do Huu, Marie-Hélène Donat, Jean Marie Duchesne, Pierre Ganil, Claude Guérémy, Eliane Honoré, Bernard Just, Roselyne Kerphirique, Sylvie Gontier, Philippe Hubert, Pierre M. Laduron, Joseph Le Blevec, Mireille Meunier, Jean-Marie Miquet, Conception Nemecek, Martine Pasquet, Odile Piot, Jeremy Pratt, Jean Rataud, Michel Reibaud, Jean-Marie Stutzmann, and Serge Mignani [Full Article - PDF]

2844-2851

Solution Structure of Iron(III)-Anthracycline Complexes Marina M. L. Fiallo, Hartmut Drechsel, Arlette Garnier-Suillerot, Berthold F. Matzanke, and Henryk Kozlowski [Full Article - PDF]

2852-2861

Synthesis and in Vivo Evaluation of New Contrast Agents for Cardiac MRI Nada H. Saab-Ismail, Tamás Simor, Balázs Gaszner, Tamás Lóránd, Márta Szöllösy, and Gabriel A. Elgavish [Full Article - PDF]

2862-2869

Hydroxylated Decahydroquinolines as Ligands for the Vesicular Acetylcholine Transporter: Synthesis and Biological Evaluation Simon M. N. Efange, Anil B. Khare, Robert H. Mach, and Stanley M. Parsons [Full Article - PDF]

2870-2880

2,3-Dihydro-2-oxo-1H-benzimidazole-1-carboxamides with Selective Affinity for the 5-HT4 Receptor: Synthesis and Structure-Affinity and Structure-Activity Relationships of a New Series of Partial Agonist and Antagonist Derivatives Inés Tapia, Luisa Alonso-Cires, Pedro Luis López-Tudanca, Ramón Mosquera, Luis Labeaga, Ana Innerárity, and Aurelio Orjales [Full Article - PDF]

2881-2886

Evaluation of the Desferrithiocin Pharmacophore as a Vector for Hydroxamates Raymond J. Bergeron, James S. McManis, Jörg Bussenius, Gary M. Brittenham, and Jan Wiegand [Full Article - PDF]

2887-2900

The Hidden Component of Size in Two-Dimensional Fragment Descriptors: Side Effects on Sampling in Bioactive Libraries Steven L. Dixon and Ryan T. Koehler [Full Article - PDF]

2901-2908

Nucleosides and Nucleotides. 185. Synthesis and Biological Activities of 4'-C-Branched-Chain Sugar Pyrimidine Nucleosides Makoto Nomura, Satoshi Shuto, Motohiro Tanaka, Takuma Sasaki, Shuichi Mori, Shiro Shigeta, and Akira Matsuda [Full Article - PDF]

2909-2919

Paullones, a Series of Cyclin-Dependent Kinase Inhibitors: Synthesis, Evaluation of CDK1/Cyclin B Inhibition, and in Vitro Antitumor Activity Christiane Schultz, Andreas Link, Maryse Leost, Daniel W. Zaharevitz, Rick Gussio, Edward A. Sausville, Laurent Meijer, and Conrad Kunick [Full Article - PDF]

2920-2926

Anti-Helicobacter pylori Agents. 3. 2-[(Arylalkyl)guanidino]-4-furylthiazoles Yousuke Katsura, Shigetaka Nishino, Mitsuko Ohno, Kazuo Sakane, Yoshimi Matsumoto, Chizu Morinaga, Hirohumi Ishikawa, and Hisashi Takasugi [Full Article - PDF]

2927-2935

Substitution at the F-Ring N-Imide of the Indolocarbazole Antitumor Drug NB-506 Increases the Cytotoxicity, DNA Binding, and Topoisomerase I Inhibition Activities Christian Bailly, Xiaogang Qu, Jonathan B. Chaires, Pierre Colson, Claude Houssier, Mitsuru Ohkubo, Susumu Nishimura, and Tomoko Yoshinari [Full Article - PDF]

2936-2945

Synthesis and Biological Activity of (Hydroxymethyl)- and (Diethylaminomethyl)benzopsoralens Adriana Chilin, Cristina Marzano, Adriano Guiotto, Paolo Manzini, Francarosa Baccichetti, Francesco Carlassare, and Franco Bordin [Full Article - PDF]

2946-2960

Synthesis and Antitumor Activity of Duocarmycin Derivatives: Modification of Segment-A of A-Ring Pyrrole Compounds Nobuyoshi Amishiro, Akihiko Okamoto, Chikara Murakata, Tatsuya Tamaoki, Masami Okabe, and Hiromitsu Saito [Full Article - PDF]

2961-2968

Structure-Activity Relationships in 1,4-Benzodioxan-Related Compounds. 6. Role of the Dioxane Unit on Selectivity for 1-Adrenoreceptor Subtypes Wilma Quaglia, Maria Pigini, Alessandro Piergentili, Mario Giannella, Gabriella Marucci, Elena Poggesi, Amedeo Leonardi, and Carlo Melchiorre [Full Article - PDF]

2969-2976

4-Heterocyclohexanone-Based Inhibitors of the Serine Protease Plasmin Tanya C. Sanders and Christopher T. Seto [Full Article - PDF]

2977-2987

Synthesis and Dopamine Receptor Modulating Activity of Substituted Bicyclic Thiazolidine Lactam Peptidomimetics of L-Prolyl-L-leucyl-glycinamide Ehab M. Khalil, Ashish Pradhan, William H. Ojala, William B. Gleason, Ram K. Mishra, and Rodney L. Johnson [Full Article - PDF]

2988-2992

Improved in Vivo Stability of Actinium-225 Macrocyclic Complexes Kim A. Deal, Ila A. Davis, Saed Mirzadeh, Stephen J. Kennel, and Martin W. Brechbiel [Full Article - PDF]

2993-3000

4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: A Novel, Potent, and Selective NR1/2B NMDA Receptor Antagonist Zhang-Lin Zhou, Sui Xiong Cai, Edward R. Whittemore, Christopher S. Konkoy, Stephen A. Espitia, Minhtam Tran, David M. Rock, Linda L. Coughenour, Jon E. Hawkinson, Peter A. Boxer, Christopher F. Bigge, Lawrence D. Wise, Eckard Weber, Richard M. Woodward, and John F. W. Keana [Full Article - PDF]

3001-3003

Synthesis and Histone Deacetylase Inhibitory Activity of New Benzamide Derivatives Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, and Nobuyuki Fukazawa , Akiko Saito, Yukiyasu Mariko, Takashi Yamashita, and Osamu Nakanishi [Full Article - PDF]

3004-3007

Importance of the Aromatic Residue at Position 6 of [Nle10]Neurokinin A(4-10) for Binding to the NK-2 Receptor and Receptor Activation Dmitry S. Gembitsky, Mark Murnin, Ferenc L. Ötvös, James Allen, Richard F. Murphy, and Sándor Lovas [Full Article - PDF]

3008-3008

Emerging Drugs: The Prospect for Improved Medicines Edited by Andrew Lynch. Ashley Publications, Ltd., London. 1999. 365 pp. 21 x 28 cm. ISSN 1361-9195. $865.00. Manfred E. Wolff [Full Article - PDF]

3008-3009

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 x 24 cm. ISBN 0-8247-1058-4. $165.00. Pat N. Confalone [Full Article - PDF]

3009-3009

Molecular Modeling of Nucleic Acids Edited by Neocles B. Leontis and John SantaLucia, Jr. ACS Symposium Series 682. American Chemical Society, Washington, D.C. 1998. x + 435 pp. 15.5 x 23.5 cm. ISBN 0-8412-3541-4. $129.95. Donald B. Boyd [Full Article - PDF]

3009-3010

Neuronal Nicotinic Receptors. Pharmacology and Therapeutics Opportunities Edited by Stephen P. Arneric and Jorge D. Brioni. Wiley-Liss, Inc., New York. 1999. xii + 421 pp. 16 x 24 cm. ISBN 0-471-24743-X. $175.00. Allan C. Collins [Full Article - PDF]