Journal of Medicinal Chemistry
Volume 42, Issue 4 (February 25, 1999)
Copyright © 1999 American Chemical Society

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COMMUNICATIONS TO THE EDITOR

533-535

Tetrahydrobenzindoles: Selective Antagonists of the 5-HT7 Receptor Chika Kikuchi, Hiroshi Nagaso, Toyokazu Hiranuma, and Masao Koyama [Full Article - PDF]

536-540

Major Groove Binding and 'DNA-Induced' Fit in the Intercalation of a Derivative of the Mixed Topoisomerase I/II Poison N-(2-(Dimethylamino)ethyl)acridine-4- carboxamide (DACA) into DNA: X-ray Structure Complexed to d(CG(5-BrU)ACG)2 at 1.3-Å Resolution Alan K. Todd, Adrienne Adams, James H. Thorpe, William A. Denny, Laurence P. G. Wakelin, and Christine J. Cardin [Full Article - PDF]

541-544

Dual Inhibition of Phosphodiesterase 4 and Matrix Metalloproteinases by an (Arylsulfonyl)hydroxamic Acid Template Robert D. Groneberg, Christopher J. Burns, Matthew M. Morrissette, John W. Ullrich, Robert L. Morris, Shelley Darnbrough, Stevan W. Djuric, Stephen M. Condon, Gerard M. McGeehan, Richard Labaudiniere, Kent Neuenschwander, Anthony C. Scotese, and Jane A. Kline [Full Article - PDF]

ARTICLES

545-559

Conformational Preferences in a Benzodiazepine Series of Potent Nonpeptide Fibrinogen Receptor Antagonists Richard M. Keenan, James F. Callahan, James M. Samanen, William E. Bondinell, Raul R. Calvo, Lichong Chen, Charles DeBrosse, Drake S. Eggleston, R. Curtis Haltiwanger, Shing Mei Hwang, Dalia R. Jakas, Thomas W. Ku, William H. Miller, Kenneth A. Newlander, Andrew Nichols, Michael F. Parker, Linda S. Southhall, Irene Uzinskas, Janice A. Vasko-Moser, Joseph W. Venslavsky, Angela S. Wong, and William F. Huffman [Full Article - PDF]

560-572

New Peptidic Cysteine Protease Inhibitors Derived from the Electrophilic -Amino Acid Aziridine-2,3-dicarboxylic Acid Tanja Schirmeister [Full Article - PDF]

573-583

Self-Organizing Molecular Field Analysis: A Tool for Structure-Activity Studies Daniel D. Robinson, Peter J. Winn, Paul D. Lyne, and W. Graham Richards [Full Article - PDF]

584-592

Syntheses and Biological Activities of Rebeccamycin Analogues. Introduction of a Halogenoacetyl Substituent Pascale Moreau, Fabrice Anizon, Martine Sancelme, Michelle Prudhomme, Christian Bailly, Danièle Sevère, Jean-François Riou, Doriano Fabbro, Thomas Meyer, and Anne-Marie Aubertin [Full Article - PDF]

593-600

Development of Chiral N-Alkylcarbamates as New Leads for Potent and Selective H3-Receptor Antagonists: Synthesis, Capillary Electrophoresis, and in Vitro and Oral in Vivo Activity Astrid Sasse, Katarzyna Kiec-Kononowicz, Holger Stark, Malgorzata Motyl, Sibylle Reidemeister, C. Robin Ganellin, Xavier Ligneau, Jean-Charles Schwartz, and Walter Schunack [Full Article - PDF]

601-608

Bicyclic Tripeptide Mimetics with Reverse Turn Inducing Properties Petra Johannesson, Gunnar Lindeberg, Weimin Tong, Adolf Gogoll, Anders Karlén, and Anders Hallberg [Full Article - PDF]

609-618

Design and Synthesis of Novel Amphiphilic Dendritic Galactosides for Selective Targeting of Liposomes to the Hepatic Asialoglycoprotein Receptor Leo A. J. M. Sliedregt, Patrick C. N. Rensen, Erik T. Rump, Peter J. van Santbrink, Martin K. Bijsterbosch, A. Rob P. M. Valentijn, Gijs A. van der Marel, Jacques H. van Boom, Theo J. C. van Berkel, and Erik A. L. Biessen [Full Article - PDF]

619-627

5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3,4-dihydropyrimidin-4(3H)-ones: Novel Potent and Selective Dihydro-alkoxy-benzyl-oxopyrimidine Derivatives Antonello Mai, Marino Artico, Gianluca Sbardella, Silvio Massa, Ettore Novellino, Giovanni Greco, Anna Giulia Loi, Enzo Tramontano, Maria Elena Marongiu, and Paolo La Colla [Full Article - PDF]

628-637

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

638-648

New N-(Pyridin-4-yl)-(indol-3-yl)acetamides and Propanamides as Antiallergic Agents Cecilia Menciu, Muriel Duflos, Fabienne Fouchard, Guillaume Le Baut, Peter Emig, Ute Achterrath, Istvan Szelenyi, Bernd Nickel, Jürgen Schmidt, Bernhard Kutscher, and Eckhardt Günther [Full Article - PDF]

649-658

Synthesis of 1-Substituted 3-(Chloromethyl)-6-aminoindoline (6-Amino-seco-CI) DNA Minor Groove Alkylating Agents and Structure-Activity Relationships for Their Cytotoxicity Jared B. J. Milbank, Moana Tercel, Graham J. Atwell, William R. Wilson, Alison Hogg, and William A. Denny [Full Article - PDF]

659-668

Cycloalkanecarboxylic Esters Derived from Lysergol, Dihydrolysergol-I, and Elymoclavine as Partial Agonists and Antagonists at Rat 5-HT2A Receptors: Pharmacological Evidence that the Indolo[4,3-fg]quinoline System of the Ergolines Is Responsible for High 5-HT2A Receptor Affinity Heinz H. Pertz, H.-Christian Milhahn, and Eckart Eich [Full Article - PDF]

669-676

New Water-Soluble Duocarmycin Derivatives: Synthesis and Antitumor Activity of A-Ring Pyrrole Compounds Bearing -Heteroarylacryloyl Groups Nobuyoshi Amishiro, Satoru Nagamura, Eiji Kobayashi, Katsushige Gomi, and Hiromitsu Saito [Full Article - PDF]

677-690

Synthesis and Serotonergic Activity of 3-[2-(Pyrrolidin-1-yl)ethyl]indoles: Potent Agonists for the h5-HT1D Receptor with High Selectivity over the h5-HT1B Receptor Francine Sternfeld, Alexander R. Guiblin, Richard A. Jelley, Victor G. Matassa, Austin J. Reeve, Peter A. Hunt, Margaret S. Beer, Anne Heald, Josephine A. Stanton, Bindi Sohal, Alan P. Watt, and Leslie J. Street [Full Article - PDF]

691-705

3-(Piperazinylpropyl)indoles: Selective, Orally Bioavailable h5-HT1D Receptor Agonists as Potential Antimigraine Agents Mark S. Chambers, Leslie J. Street, Simon Goodacre, Sarah C. Hobbs, Peter Hunt, Richard A. Jelley, Victor G. Matassa, Austin J. Reeve, Francine Sternfeld, Margaret S. Beer, Josephine A. Stanton, Denise Rathbone, Alan P. Watt, and Angus M. MacLeod [Full Article - PDF]

706-721

Synthesis, CoMFA Analysis, and Receptor Docking of 3,5-Diacyl-2,4-Dialkylpyridine Derivatives as Selective A3 Adenosine Receptor Antagonists An-Hu Li, Stefano Moro, Nancy Forsyth, Neli Melman, Xiao-duo Ji, and Kenneth A. Jacobson [Full Article - PDF]

722-729

Phosphotyrosine-Containing Dipeptides as High-Affinity Ligands for the p56lck SH2 Domain Montse Llinàs-Brunet, Pierre L. Beaulieu, Dale R. Cameron, Jean-Marie Ferland, Jean Gauthier, Elise Ghiro, James Gillard, Vida Gorys, Martin Poirier, Jean Rancourt, and Dominik Wernic , Raj Betageri, Mario Cardozo, Scott Jakes, Suzanne Lukas, Usha Patel, John Proudfoot, and Neil Moss [Full Article - PDF]

730-741

Aminopyridazines as Acetylcholinesterase Inhibitors Jean-Marie Contreras, Yveline M. Rival, Said Chayer, Jean-Jacques Bourguignon, and Camille G. Wermuth [Full Article - PDF]

742-750

Synthesis of Retinoid X Receptor-Specific Ligands That Are Potent Inducers of Adipogenesis in 3T3-L1 Cells Stacie S. Canan Koch, Laura J. Dardashti, Rosemary M. Cesario, Glenn E. Croston, Marcus F. Boehm, Richard A. Heyman, and Alex M. Nadzan [Full Article - PDF]

751-760

Synthesis of Novel 2-Benzothiopyran and 3-Benzothiepin Derivatives and Their Stimulatory Effect on Bone Formation Tsuneo Oda, Kohei Notoya, Masayuki Gotoh, Shigehisa Taketomi, Yukio Fujisawa, Haruhiko Makino, and Takashi Sohda [Full Article - PDF]

761-768

Corticotropin Releasing Factor (CRF) Agonists with Reduced Amide Bonds and Ser7 Substitutions Laura Cervini, Paula Theobald, Anne Corrigan, A. Grey Craig, Catherine Rivier, Wylie Vale, and Jean Rivier [Full Article - PDF]

BRIEF ARTICLES

769-776

Structure-Activity Relationships of Pyrazole Derivatives as Cannabinoid Receptor Antagonists Ruoxi Lan, Qian Liu, Pusheng Fan, Sonyuan Lin, Susanthi R. Fernando, Deirdre McCallion, Roger Pertwee, and Alexandros Makriyannis [Full Article - PDF]

BOOK REVIEWS

777-777

Heparin-Binding Proteins By H. Edward Conrad. Academic Press, San Diego, CA, and London. 1998. xvi + 527 pp. 16 x 23.5 cm. ISBN 0-12-186060-4. $89.95. Ulf Lindahl [Full Article - PDF]

777-778

Comparative QSAR Edited by James Devillers. Taylor and Francis, Washington, DC. 1998. ix + 371 pp. 16 × 24 cm. ISBN 1-56032-716-2. $135.00. Yvonne C. Martin [Full Article - PDF]