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3339-3342
Discovery of 4-[(Z)-(4-Bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-Oxide (SCH 351125): An Orally Bioavailable Human CCR5 Antagonist for the Treatment of HIV Infection
Anandan Palani,
Sherry Shapiro,
John W. Clader,
William J. Greenlee,
Kathleen Cox,
Julie Strizki,
Michael Endres, and
Bahige M. Baroudy
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3343-3346
Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. II. Discovery of 1-[(2,4-Dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoro- methyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-Oxide (Sch-350634), an Orally Bioavailable, Potent CCR5 Antagonist
Jayaram R. Tagat,
Ruo W. Steensma,
Stuart W. McCombie,
Dennis V. Nazareno,
Sue-Ing Lin,
Bernard R. Neustadt,
Kathleen Cox,
Serena Xu,
Lisa Wojcik,
Michael G. Murray,
Nicole Vantuno,
Bahige M. Baroudy, and
Julie M. Strizki
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3347-3350
Design and Synthesis of a Series of (2R)-N4-Hydroxy-2-(3-hydroxybenzyl)-N- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden- 1-yl]butanediamide Derivatives as Potent, Selective, and Orally Bioavailable Aggrecanase Inhibitors
Wenqing Yao,
Zelda R. Wasserman,
Michael Chao,
Gade Reddy,
Eric Shi,
Rui-Qin Liu,
Maryanne B. Covington,
Elizabeth C. Arner,
Michael A. Pratta,
Micky Tortorella,
Ronald L. Magolda,
Robert Newton,
MingXin Qian,
Maria D. Ribadeneira,
David Christ,
Ruth R. Wexler, and
Carl P. Decicco
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3351-3354
Discovery of Macrocyclic Hydroxamic Acids Containing Biphenylmethyl Derivatives at P1', a Series of Selective TNF- Converting Enzyme Inhibitors with Potent Cellular Activity in the Inhibition of TNF- Release
Chu-Biao Xue,
Xiaohua He,
Ronald L. Corbett,
John Roderick,
Zelda R. Wasserman,
Rui-Qin Liu,
Bruce D. Jaffee,
Maryanne B. Covington,
Mingxin Qian,
James M. Trzaskos,
Robert C. Newton,
Ronald L. Magolda,
Ruth R. Wexler, and
Carl P. Decicco
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3355-3368
Potent and Selective ET-A Antagonists. 1. Syntheses and Structure-Activity Relationships of N-(6-(2-(Aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide Derivatives
Hiroshi Morimoto,
Hideshi Shimadzu,
Emi Kushiyama,
Hiroyuki Kawanishi,
Toshihiro Hosaka,
Yasushi Kawase,
Kosuke Yasuda,
Kohei Kikkawa,
Rikako Yamauchi-Kohno, and
Koichiro Yamada
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3369-3377
Potent and Selective ET-A Antagonists. 2. Discovery and Evaluation of Potent and Water Soluble N-(6-(2-(Aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide Derivatives
Hiroshi Morimoto,
Noriko Ohashi,
Hideshi Shimadzu,
Emi Kushiyama,
Hiroyuki Kawanishi,
Toshihiro Hosaka,
Yasushi Kawase,
Kosuke Yasuda,
Kohei Kikkawa,
Rikako Yamauchi-Kohno, and
Koichiro Yamada
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3378-3390
From Hit to Lead. Combining Two Complementary Methods for Focused Library Design. Application to  Opiate Ligands
Rébecca Poulain,
Dragos Horvath,
Béatrice Bonnet,
Christian Eckhoff,
Béatrice Chapelain,
Marie-Christine Bodinier, and
Benoît Déprez
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3391-3401
From Hit to Lead. Analyzing Structure-Profile Relationships
Rébecca Poulain,
Dragos Horvath,
Béatrice Bonnet,
Christian Eckhoff,
Béatrice Chapelain,
Marie-Christine Bodinier, and
Benoît Déprez
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3402-3406
Synthesis of Potent C2-Symmetric, Diol-Based HIV-1 Protease Inhibitors. Investigation of Thioalkyl and Thioaryl P1/P1' Substituents
Anna Mühlman,
Björn Classon,
Anders Hallberg, and
Bertil Samuelsson
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3407-3416
Synthesis of Novel, Potent, Diol-Based HIV-1 Protease Inhibitors via Intermolecular Pinacol Homocoupling of (2S)-2-Benzyloxymethyl-4-phenylbutanal
Anna Mühlman,
Jimmy Lindberg,
Björn Classon,
Torsten Unge,
Anders Hallberg, and
Bertil Samuelsson
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3417-3423
Are Free Energy Calculations Useful in Practice? A Comparison with Rapid Scoring Functions for the p38 MAP Kinase Protein System
David A. Pearlman and
Paul S. Charifson
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3424-3439
Statistical Molecular Design, Parallel Synthesis, and Biological Evaluation of a Library of Thrombin Inhibitors
Anna Linusson,
Johan Gottfries,
Thomas Olsson,
Eivor Örnskov,
Staffan Folestad,
Bo Nordén, and
Svante Wold
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3440-3452
Synthesis and Biological Evaluation of s-Triazine Substituted Polyamines as Potential New Anti-Trypanosomal Drugs
Burkhard Klenke,
Mhairi Stewart,
Michael P. Barrett,
Reto Brun, and
Ian H. Gilbert
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3453-3462
Synthesis, DNA Cross-Linking Activity, and Cytotoxicity of Dimeric Mitomycins
Younghwa Na,
Ven-Shun Li,
Yuka Nakanishi,
Kenneth F. Bastow, and
Harold Kohn
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3463-3468
A New Class of Ibuprofen Derivatives with Reduced Gastrotoxicity
Marco L. Lolli,
Clara Cena,
Claudio Medana,
Loretta Lazzarato,
Giuseppina Morini,
Gabriella Coruzzi,
Stefano Manarini,
Roberta Fruttero, and
Alberto Gasco
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3469-3487
Selective Inhibition of ICAM-1 and E-Selectin Expression in Human Endothelial Cells. 2. Aryl Modifications of 4-(Aryloxy)thieno[2,3-c]pyridines with Fine-Tuning at C-2 Carbamides
Gui-Dong Zhu,
David L. Arendsen,
Indrani W. Gunawardana,
Steven A. Boyd,
Andrew O. Stewart,
Dennis G. Fry,
Barbara L. Cool,
Lemma Kifle,
Verlyn Schaefer,
Joseph Meuth,
Kennan C. Marsh,
Anita J. Kempf-Grote,
Patrick Kilgannon,
W. Michael Gallatin, and
Gregory F. Okasinski
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3488-3503
1,2-Benzothiazine 1,1-Dioxide P2-P3 Peptide Mimetic Aldehyde Calpain I Inhibitors
Gregory J. Wells,
Ming Tao,
Kurt A. Josef, and
Ron Bihovsky
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3504-3510
Palmitoyl Derivatives of GpMBP Epitopes: T-Cell Response and Peptidases Susceptibility
Anna M. Papini,
Benedetta Mazzanti,
Elena Nardi,
Elisabetta Traggiai,
Clara Ballerini,
Tiziana Biagioli,
Hubert Kalbacher,
Hermann Beck,
Martin Deeg,
Mario Chelli,
Mauro Ginanneschi,
Luca Massacesi, and
Marco Vergelli
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3511-3522
Hypoxia-Selective Antitumor Agents. 16. Nitroarylmethyl Quaternary Salts as Bioreductive Prodrugs of the Alkylating Agent Mechlorethamine
Moana Tercel,
Alan E. Lee,
Alison Hogg,
Robert F. Anderson,
Ho H. Lee,
Bronwyn G. Siim,
William A. Denny, and
William R. Wilson
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3523-3530
Long Lasting Antinociceptive Properties of Enkephalin Degrading Enzyme (NEP and APN) Inhibitor Prodrugs
Huixiong Chen,
Florence Noble,
Bernard P. Roques, and
Marie-Claude Fournié-Zaluski
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3531-3538
Synthesis and Antiviral Activity of Novel 5-(1-Cyanamido-2-haloethyl) and 5-(1-Hydroxy(or methoxy)-2-azidoethyl) Analogues of Uracil Nucleosides
Rakesh Kumar,
Dinesh Rai,
Sanjay K. Sharma,
Holly A. Saffran,
Ryan Blush, and
D. Lorne J. Tyrrell
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3539-3539
| Analytical Chemistry in a GMP Environment: A Practical Guide Edited by James M. Miller and Jonathan B. Crowther. John Wiley & Sons, Inc., New York. 2000. xxiv + 488 pp. 16 × 24 cm. ISBN 0-471-31431-5. $115.00.
S. Alta Botha
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3539-3539
| Solid-Phase Organic Synthesis. Volume 1 Edited by Anthony W. Czarnik. John Wiley & Sons, New York. 2001. viii + 164 pp. 16 × 23.5 cm. ISBN 0-471-31484-6. $69.95.
Thomas J. Sowin
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