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PERSPECTIVES
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527-550
| The PPARs: From Orphan Receptors to Drug Discovery
Timothy M. Willson,
Peter J. Brown,
Daniel D. Sternbach, and
Brad R. Henke
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EXPEDITED ARTICLES
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551-559
Novel Ligands Lacking a Positive Charge for the  - and  -Opioid Receptors
Peter W. Schiller,
Irena Berezowska,
Thi M.-D. Nguyen,
Ralf Schmidt,
Carole Lemieux,
Nga N. Chung,
Margaret L. Falcone-Hindley,
Wenqing Yao,
Josephine Liu,
Seiji Iwama,
Amos B. Smith, III, and
Ralph Hirschmann
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ARTICLES
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560-568
Phenyl  -Methoxyacrylates: A New Antimalarial Pharmacophore
Jawad Alzeer,
Jacques Chollet,
Ingrid Heinze-Krauss,
Christian Hubschwerlen,
Hugues Matile, and
Robert G. Ridley
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569-580
Opiate Aromatic Pharmacophore Structure-Activity Relationships in CTAP Analogues Determined by Topographical Bias, Two-Dimensional NMR, and Biological Activity Assays
G. Gregg Bonner,
Peg Davis,
Dagmar Stropova,
Sidney Edsall,
Henry I. Yamamura,
Frank Porreca, and
Victor J. Hruby
[Abstract][Full Text - HTML][Full Article - PDF][Purchase Article][Supporting Information]
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581-590
Chiral Nonsteroidal Affinity Ligands for the Androgen Receptor. 1. Bicalutamide Analogues Bearing Electrophilic Groups in the B Aromatic Ring
Leonid Kirkovsky,
Arnab Mukherjee,
Donghua Yin,
James T. Dalton, and
Duane D. Miller
[Abstract][Full Text - HTML][Full Article - PDF][Purchase Article]
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591-598
Synthesis and Human -Adrenoceptor Activity of 1-(3,5-Diiodo-4- methoxybenzyl)-1,2,3,4-tetrahydroisoquinolin-6-ol Derivatives in Vitro
Yali He,
Victor I. Nikulin,
Sandeep S. Vansal,
Dennis R. Feller, and
Duane D. Miller
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599-608
Binding and Preliminary Evaluation of 5-Hydroxy- and 10-Hydroxy-2,3,12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines as Dopamine Receptor Ligands
Francesco Claudi,
Antonio Di Stefano,
Fabrizio Napolitani,
Gian Mario Cingolani,
Gianfabio Giorgioni,
Josè A. Fontenla,
Gisela Y. Montenegro,
Maria E. Rivas,
Elizabeth Rosa,
Barbara Michelotto,
Giustino Orlando, and
Luigi Brunetti
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609-612
Hypocholesterolemic and Hypolipidemic Activity of Some Novel Morpholine Derivatives with Antioxidant Activity
Michael C. Chrysselis,
Eleni A. Rekka, and
Panos N. Kourounakis
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613-628
Steroidal Affinity Labels of the Estrogen Receptor  . 4. Electrophilic 11-Aryl Derivatives of Estradiol
Sigrid Aliau,
Georges Delettre,
Hélène Mattras,
Driss El Garrouj,
François Nique,
Georges Teutsch, and
Jean-Louis Borgna
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629-638
Inhibitors of Topoisomerase II Based on the Benzodiimidazole and Dipyrroloimidazobenzimidazole Ring Systems: Controlling DT-Diaphorase Reductive Inactivation with Steric Bulk
William G. Schulz and
Edward B. Skibo
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639-648
Synthesis, Biodistribution, and Primate Imaging of Fluorine-18 Labeled 2-Carbo-1'-fluoro-2-propoxy-3-(4-chlorophenyl)tropanes. Ligands for the Imaging of Dopamine Transporters by Positron Emission Tomography
Dongxia Xing,
Ping Chen,
Robert Keil,
Clinton D. Kilts,
Bing Shi,
Vernon M. Camp,
Gene Malveaux,
Timothy Ely,
Michael J. Owens,
John Votaw,
Margaret Davis,
John M. Hoffman,
Roy A. E. BaKay,
Thygarajan Subramanian,
Ray L. Watts, and
Mark M. Goodman
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649-663
Diamino Benzo[b]thiophene Derivatives as a Novel Class of Active Site Directed Thrombin Inhibitors. 5. Potency, Efficacy, and Pharmacokinetic Properties of Modified C-3 Side Chain Derivatives
Daniel J. Sall,
Dianna L. Bailey,
Jolie A. Bastian,
John A. Buben,
Nickolay Y. Chirgadze,
Amy C. Clemens-Smith,
Michael L. Denney,
Matthew J. Fisher,
Deborah D. Giera,
Donetta S. Gifford-Moore,
Richard W. Harper,
Lea M. Johnson,
Valentine J. Klimkowski,
Todd J. Kohn,
Ho-Shen Lin,
Jefferson R. McCowan,
Alan D. Palkowitz,
Michael E. Richett,
Gerald F. Smith,
David W. Snyder,
Kumiko Takeuchi,
John E. Toth, and
Minsheng Zhang
[Abstract][Full Text - HTML][Full Article - PDF][Purchase Article][Supporting Information]
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664-674
Inhibitors of Tripeptidyl Peptidase II. 2. Generation of the First Novel Lead Inhibitor of Cholecystokinin-8-Inactivating Peptidase: A Strategy for the Design of Peptidase Inhibitors
C. Robin Ganellin,
Paul B. Bishop,
Ramesh B. Bambal,
Suzanne M. T. Chan,
James K. Law,
Benoit Marabout,
Pratibha Mehta Luthra,
Andrew N. J. Moore,
Olivier Peschard,
Pierre Bourgeat,
Christiane Rose,
Froylan Vargas, and
Jean-Charles Schwartz
[Abstract][Full Text - HTML][Full Article - PDF][Purchase Article][Supporting Information]
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675-682
Palladium-Catalyzed Cross-Coupling Reactions for the Synthesis of 6,8-Disubstituted 1,7-Naphthyridines: A Novel Class of Potent and Selective Phosphodiesterase Type 4D Inhibitors
Rene Hersperger,
Katharine Bray-French,
Lazzaro Mazzoni, and
Thomas Müller
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683-689
Benzyl Derivatives of 2,1,3-Benzo- and Benzothieno[3,2-a]thiadiazine 2,2-Dioxides: First Phosphodiesterase 7 Inhibitors
Ana Martínez,
Ana Castro,
Carmen Gil,
Montserrat Miralpeix,
Victor Segarra,
Teresa Doménech,
Jorge Beleta,
Jose M. Palacios,
Hamish Ryder,
Xavier Miró,
Carles Bonet,
Josep M. Casacuberta,
Ferran Azorín,
Benjamí Piña, and
Pere Puigdoménech
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690-705
Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic Acids as Leukotriene Biosynthesis Inhibitors
Teodozyj Kolasa,
David E. Gunn,
Pramila Bhatia,
Keith W. Woods,
Todd Gane,
Andrew O. Stewart,
Jennifer B. Bouska,
Richard R. Harris,
Keren I. Hulkower,
Peter E. Malo,
Randy L. Bell,
George W. Carter, and
Clint D. W. Brooks
[Abstract][Full Text - HTML][Full Article - PDF][Purchase Article][Supporting Information]
| |
706-720
A New Class of Conformationally Rigid Analogues of 4-Amino-5-halopentanoic Acids, Potent Inactivators of  -Aminobutyric Acid Aminotransferase
Jian Qiu and
Richard B. Silverman
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721-735
Structure-Activity Relationship Studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a Potent Inhibitor of Leukotriene A4 (LTA4) Hydrolase
Thomas D. Penning,
Nizal S. Chandrakumar,
Barbara B. Chen,
Helen Y. Chen,
Bipin N. Desai,
Stevan W. Djuric,
Stephen H. Docter,
Alan F. Gasiecki,
Richard A. Haack,
Julie M. Miyashiro,
Mark A. Russell,
Stella S. Yu,
David G. Corley,
Richard C. Durley,
Brian F. Kilpatrick,
Barry L. Parnas,
Leslie J. Askonas,
James K. Gierse,
Elizabeth I. Harding,
Maureen K. Highkin,
James F. Kachur,
Suzanne H. Kim,
Gwen G. Krivi,
Doreen Villani-Price,
E. Yvonne Pyla,
Walter G. Smith, and
Nayereh S. Ghoreishi-Haack
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736-745
The Cyclohexene Ring System as a Furanose Mimic: Synthesis and Antiviral Activity of Both Enantiomers of Cyclohexenylguanine
Jing Wang,
Matheus Froeyen,
Chris Hendrix,
Graciela Andrei,
Robert Snoeck,
Erik De Clercq, and
Piet Herdewijn
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746-755
Acyclic Analogues of Deoxyadenosine 3',5'-Bisphosphates as P2Y1 Receptor Antagonists
Yong-Chul Kim,
Carola Gallo-Rodriguez,
Soo-Yeon Jang,
Erathodiyil Nandanan,
Mary Adams,
T. Kendall Harden,
José L. Boyer, and
Kenneth A. Jacobson
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BRIEF ARTICLES
|
756-762
Conjugated Enynes as Nonaromatic Catechol Bioisosteres: Synthesis, Binding Experiments, and Computational Studies of Novel Dopamine Receptor Agonists Recognizing Preferentially the D3 Subtype
Harald Hübner,
Christian Haubmann,
Wolfgang Utz, and
Peter Gmeiner
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BOOK REVIEWS
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763-763
| Drugs and the Pharmaceutical Sciences. Volume 100. New Drug Approval Process, 3rd Edition Edited by Richard A. Guarino. Marcel Dekker, Inc., New York. 1999. xxxiii + 471 pp. 16 × 23.5 cm. ISBN 0-8247-0308-1. $185.00.
Bruce Ronsen
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ADDITIONS AND CORRECTIONS
|
764-764
|
Asim Kumar Debnath: Three-Dimensional Quantitative Structure-Activity Relationship Study on Cyclic
Urea Derivatives as HIV-1 Protease Inhibitors: Application of Comparative Molecular Field Analysis.
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