|
PERSPECTIVES
|
1641-1660
| Corticotropin Releasing Factor (CRF) Receptor Modulators: Progress and Opportunities for New Therapeutic Agents
Paul J. Gilligan,
David W. Robertson, and
Robert Zaczek
[Full Article -
PDF] | |
COMMUNICATIONS
|
1661-1663
N-[[(5-Methyl-3-phenylisoxazol-4-yl)- phenyl]sulfonyl]propanamide, Sodium Salt, Parecoxib Sodium: A Potent and Selective Inhibitor of COX-2 for Parenteral Administration
John J. Talley,
Stephen R. Bertenshaw,
David L. Brown,
Jeffery S. Carter,
Matthew J. Graneto,
Michael S. Kellogg,
Carol M. Koboldt,
Jinhua Yuan,
Yan Y. Zhang, and
Karen Seibert
[Full Article -
PDF]
| |
EXPEDITED ARTICLES
|
1664-1669
Potent Derivatives of Glucagon-like Peptide-1 with Pharmacokinetic Properties Suitable for Once Daily Administration
Lotte B. Knudsen,
Per F. Nielsen,
Per O. Huusfeldt,
Nils L. Johansen,
Kjeld Madsen,
Freddy Z. Pedersen,
Henning Th gersen,
Michael Wilken, and
Henrik Agers
[Full Article -
PDF]
| |
ARTICLES
|
1670-1683
Substituted Benzamide Inhibitors of Human Rhinovirus 3C Protease: Structure-Based Design, Synthesis, and Biological Evaluation
Siegfried H. Reich,
Theodore Johnson,
Michael B. Wallace,
Susan E. Kephart,
Shella A. Fuhrman,
Stephen T. Worland,
David A. Matthews,
Thomas F. Hendrickson,
Fora Chan,
James Meador, III,
Rose Ann Ferre,
Edward L. Brown,
Dorothy M. DeLisle,
Amy K. Patick,
Susan L. Binford, and
Clifford E. Ford
[Full Article -
PDF]
| |
1684-1691
Molecular Determinants of MAO Selectivity in a Series of Indolylmethylamine Derivatives: Biological Activities, 3D-QSAR/CoMFA Analysis, and Computational Simulation of Ligand Recognition
Jose A. Morón,
Mercedes Campillo,
Virgili Perez,
Mercedes Unzeta, and
Leonardo Pardo
[Full Article -
PDF]
| |
1692-1698
Probing the Conformation of the Sugar Transport Inhibitor Phlorizin by 2D-NMR, Molecular Dynamics Studies, and Pharmacophore Analysis
Susanne Wielert-Badt,
Jiann-Trzuo Lin,
Mike Lorenz,
Stefan Fritz, and
Rolf K.-H. Kinne
[Full Article -
PDF]
| |
1699-1704
2-Amino-2-oxazolines as Subtype Selective 2 Adrenoceptor Agonists
Wai C. Wong,
Wanying Sun,
Weili Cui,
Yuewen Chen,
Carlos Forray,
Pierre J.-J. Vaysse,
Theresa A. Branchek, and
Charles Gluchowski
[Full Article -
PDF]
| |
1705-1713
New Proline Mimetics: Synthesis of Thrombin Inhibitors Incorporating Cyclopentane- and Cyclopentenedicarboxylic Acid Templates in the P2 Position. Binding Conformation Investigated by X-ray Crystallography
Daniel Nöteberg,
Jonas Brånalt,
Ingemar Kvarnström,
Marcel Linschoten,
Djordje Musil,
Jan-Erik Nyström,
Guido Zuccarello, and
Bertil Samuelsson
[Full Article -
PDF]
| |
1714-1722
Design and Synthesis of Conformationally Constrained Glucagon Analogues
Dev Trivedi,
Ying Lin,
Jung-Mo Ahn,
Mara Siegel,
Nevena N. Mollova,
Karl H. Schram, and
Victor J. Hruby
[Full Article -
PDF]
| |
1723-1740
Toward General Methods of Targeted Library Design: Topomer Shape Similarity Searching with Diverse Structures as Queries
Katherine M. Andrews and
Richard D. Cramer
[Full Article -
PDF]
| |
1741-1753
Solution Structures in SDS Micelles and Functional Activity at the Bullfrog Substance P Receptor of Ranatachykinin Peptides
Shane A. Perrine,
Tracy L. Whitehead,
Rickey P. Hicks,
John L. Szarek,
James E. Krause, and
Mark A. Simmons
[Full Article -
PDF]
| |
1754-1761
Characterization of the Binding Site of the Histamine H3 Receptor. 2. Synthesis, in Vitro Pharmacology, and QSAR of a Series of Monosubstituted Benzyl Analogues of Thioperamide
Albert D. Windhorst,
Henk Timmerman,
Edward A. Worthington,
Greetje J. Bijloo,
Paul H. J. Nederkoorn,
Wiro M. P. B. Menge,
Rob Leurs, and
Jacobus D. M. Herscheid
[Full Article -
PDF]
| |
1762-1769
Screening of New Antioxidant Molecules Using Flow Cytometry
Serge Ostrovidov,
Patricia Franck,
Delphine Joseph,
Laurent Martarello,
Gilbert Kirsch,
Francine Belleville,
Pierre Nabet, and
Brigitte Dousset
[Full Article -
PDF]
| |
1770-1779
Design of a Gag Pentapeptide Analogue that Binds Human Cyclophilin A More Efficiently than the Entire Capsid Protein: New Insights for the Development of Novel Anti-HIV-1 Drugs
Quan Li,
Mireille Moutiez,
Jean-Baptiste Charbonnier,
Karine Vaudry,
André Ménez,
Eric Quéméneur, and
Christophe Dugave
[Full Article -
PDF]
| |
1780-1792
Nuclear Receptor-DNA Binding Specificity: A COMBINE and Free-Wilson QSAR Analysis
Sanja Tomic,
Lennart Nilsson, and
Rebecca C. Wade
[Full Article -
PDF]
| |
1793-1806
Protease Inhibitors: Synthesis and QSAR Study of Novel Classes of Nonbasic Thrombin Inhibitors Incorporating Sulfonylguanidine and O-Methylsulfonylisourea Moieties at P1
Claudiu T. Supuran,
Andrea Scozzafava,
Fabrizio Briganti, and
Brian W. Clare
[Full Article -
PDF]
| |
1807-1816
Multivariate Data Analysis Using D-Optimal Designs, Partial Least Squares, and Response Surface Modeling: A Directional Approach for the Analysis of Farnesyltransferase Inhibitors
Elie Giraud,
Claude Luttmann,
François Lavelle,
Jean-François Riou,
Patrick Mailliet, and
Abdelazize Laoui
[Full Article -
PDF]
| |
1817-1825
Synthesis and Cytostatic Activity of Substituted 6-Phenylpurine Bases and Nucleosides: Application of the Suzuki-Miyaura Cross-Coupling Reactions of 6-Chloropurine Derivatives with Phenylboronic Acids
Michal Hocek,
Antonín Hol ,
Ivan Votruba, and
Hana Dvo áková
[Full Article -
PDF]
| |
1826-1840
Design and Synthesis of Aryloxyethyl Thiocyanate Derivatives as Potent Inhibitors of Trypanosoma cruzi Proliferation
Sergio H. Szajnman,
Wen Yan,
Brian N. Bailey,
Roberto Docampo,
Eleonora Elhalem, and
Juan B. Rodriguez
[Full Article -
PDF]
| |
1841-1851
1-Imidazolyl(alkyl)-Substituted Di- and Tetrahydroquinolines and Analogues: Syntheses and Evaluation of Dual Inhibitors of Thromboxane A2 Synthase and Aromatase
Christoph Jacobs,
Martin Frotscher,
Gerd Dannhardt, and
Rolf W. Hartmann
[Full Article -
PDF]
| |
1852-1857
Structural Determinants of Opioid Activity in the Orvinols and Related Structures: Ethers of Orvinol and Isoorvinol
Andrew Coop,
Claire L. Norton,
Ilona Berzetei-Gurske,
Jackie Burnside,
Lawrence Toll,
Stephen M. Husbands, and
John W. Lewis
[Full Article -
PDF]
| |
1858-1865
Protease Inhibitors: Synthesis of Potent Bacterial Collagenase and Matrix Metalloproteinase Inhibitors Incorporating N-4-Nitrobenzylsulfonylglycine Hydroxamate Moieties
Andrea Scozzafava and
Claudiu T. Supuran
[Full Article -
PDF]
| |
1866-1877
Novel Synthetic Oleanane and Ursane Triterpenoids with Various Enone Functionalities in Ring A as Inhibitors of Nitric Oxide Production in Mouse Macrophages
Tadashi Honda,
Gordon W. Gribble,
Nanjoo Suh,
Heather J. Finlay,
BarbieAnn V. Rounds,
Lothar Bore,
Frank G. Favaloro, Jr.,
Yongping Wang, and
Michael B. Sporn
[Full Article -
PDF]
| |
1878-1885
Design and Synthesis of trans-N-[4-[2-(6-Cyano-1,2,3,4-tetrahydroisoquinolin-2- yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A Potent and Selective Dopamine D3 Receptor Antagonist with High Oral Bioavailability and CNS Penetration in the Rat
Geoffrey Stemp,
Tracey Ashmeade,
Clive L. Branch,
Michael S. Hadley,
A. Jacqueline Hunter,
Christopher N. Johnson,
David J. Nash,
Kevin M. Thewlis,
Antonio K. K. Vong,
Nigel E. Austin,
Phillip Jeffrey,
Kim Y. Avenell,
Izzy Boyfield,
Jim J. Hagan,
Derek N. Middlemiss,
Charlie Reavill,
Graham J. Riley,
Carole Routledge, and
Martyn Wood
[Full Article -
PDF]
| |
BRIEF ARTICLES
|
1886-1891
Structure-Based Design, Synthesis, and Biological Evaluation of Novel Pyrrolyl Aryl Sulfones: HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors Active at Nanomolar Concentrations
Marino Artico,
Romano Silvestri,
Eugenia Pagnozzi,
Biancamaria Bruno,
Ettore Novellino,
Giovanni Greco,
Silvio Massa,
Alessandro Ettorre,
Anna Giulia Loi,
Franca Scintu, and
Paolo La Colla
[Full Article -
PDF]
| |
1892-1897
Subtype-Selective N-Methyl-D-aspartate Receptor Antagonists: Benzimidazalone and Hydantoin as Phenol Replacements
Robert M. Schelkun,
Po-wai Yuen,
Kevin Serpa,
Leonard T. Meltzer, and
Lawrence D. Wise
, Edward R. Whittemore and
Richard M. Woodward
[Full Article -
PDF]
| |
BOOK REVIEWS
|
1898-1898
| Handbook of Drug Metabolism Edited by Thomas L. Woolf. Marcel Dekker, New York. 1999. xi + 596 pp. 18 x 26 cm. ISBN 0-8247-0229-8. $225.00.
D. Eric Walters
[Full Article -
PDF] | |
1898-1899
| Handbook of Reagents for Organic Synthesis. Reagents, Auxiliaries, and Catalysts for C-C Bond Formation Edited by Robert M. Coates and Scott E. Denmark. John Wiley & Sons, Inc., New York. 1999. xvi + 746 pp. 22 x 28.5 cm. ISBN 0-471-97924. $115.00. Acidic and Basic Reagents. Edited by Hans J. Reich and James H. Rigby. John Wiley & Sons, Inc., New York. 1999. xii + 494 pp. 22 x 28.5 cm. ISBN 0-471-97925. $115.00. Oxidizing and Reducing Reagents. Edited by Steven D. Burke and Rick L. Danheiser. John Wiley & Sons, Inc., New York. 1999. xviii + 550 pp. 22 x 28.5 cm. ISBN 0-471-97926-0. $115.00. Activating Agents and Protecting Groups. Edited by Anthony J. Pearson and William R. Roush. John Wiley & Sons, Inc., New York. 1999. xvii + 513 pp. 22 x 28.5 cm. ISBN 0-471-97927-9. $115.00.
Horacio F. Olivo
[Full Article -
PDF] | |
1899-1900
| Pharmaceutical Innovation. Revolutionizing Human Health Edited by Ralph Landau, Basil Achilladelis, and Alexander Scriabine. Chemical Heritage Press, Philadelphia. 1999. xxiii + 408 pp. 16 × 24 cm. ISBN 0-941901-21-1. $44.95.
Carl Kaiser
[Full Article -
PDF] | |