PERSPECTIVES
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2721-2736
Pharmacotherapies for Treatment of Cocaine Abuse: Preclinical Aspects
F. Ivy Carroll,
Leonard L. Howell, and
Michael J. Kuhar
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COMMUNICATIONS
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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
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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
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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
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ARTICLES
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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
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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
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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
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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
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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.
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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
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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
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2844-2851
Solution Structure of Iron(III)-Anthracycline Complexes
Marina M. L. Fiallo,
Hartmut Drechsel,
Arlette Garnier-Suillerot,
Berthold F. Matzanke, and
Henryk Kozlowski
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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2969-2976
4-Heterocyclohexanone-Based Inhibitors of the Serine Protease Plasmin
Tanya C. Sanders and
Christopher T. Seto
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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
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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
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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
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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
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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
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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
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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
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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
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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
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