Table of Contents

September 25, 2003
Volume 46, Issue 20
Pages 4215-4364

About the Cover: Connolly surface map of the X-ray structure of the α-thrombin-cyclopentenedicarboxylic acid derivative complex (yellow) at 1.9 Å resolution superimposed on the X-ray structure of the α-thrombin-PPACK complex (magenta) (Thorstensson, F.; et al. J. Med. Chem. 2003, 46, 1165-1179).

Award Address

Peptide Science:  Exploring the Use of Chemical Principles and Interdisciplinary Collaboration for Understanding Life Processes

pp 4215–4231
Publication Date (Web): September 04, 2003 (Perspective)
DOI: 10.1021/jm0303103

Letters

Fragment Screening and Assembly:  A Highly Efficient Approach to a Selective and Cell Active Protein Tyrosine Phosphatase 1B Inhibitor

pp 4232–4235
Publication Date (Web): September 03, 2003 (Letter)
DOI: 10.1021/jm034122o

Discovery of 4-Benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806):  A Novel HIV-1 Attachment Inhibitor That Interferes with CD4-gp120 Interactions

pp 4236–4239
Publication Date (Web): August 30, 2003 (Letter)
DOI: 10.1021/jm034082o

Oxidosqualene Cyclase Inhibitors as Antimicrobial Agents

pp 4240–4243
Publication Date (Web): August 29, 2003 (Letter)
DOI: 10.1021/jm034126t

Articles

Structure−Activity Relationships of the Antimalarial Agent Artemisinin. 8. Design, Synthesis, and CoMFA Studies toward the Development of Artemisinin-Based Drugs against Leishmaniasis and Malaria

pp 4244–4258
Publication Date (Web): August 21, 2003 (Article)
DOI: 10.1021/jm030181q

Discovery, Characterization, and Structure−Activity Relationships Studies of Proapoptotic Polyphenols Targeting B-Cell Lymphocyte/Leukemia-2 Proteins

pp 4259–4264
Publication Date (Web): August 22, 2003 (Article)
DOI: 10.1021/jm030190z

A Specific Mechanism of Nonspecific Inhibition

pp 4265–4272
Publication Date (Web): August 22, 2003 (Article)
DOI: 10.1021/jm030266r

Synthesis and Biological Characterization of 1-Methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole Derivatives as Muscarinic Agonists for the Treatment of Neurological Disorders

pp 4273–4286
Publication Date (Web): August 30, 2003 (Article)
DOI: 10.1021/jm0301235

Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine Derivatives as Adenosine Receptor Antagonists. Influence of the N5 Substituent on the Affinity at the Human A3 and A2B Adenosine Receptor Subtypes:  A Molecular Modeling Investigation

pp 4287–4296
Publication Date (Web): August 30, 2003 (Article)
DOI: 10.1021/jm030852k

Synthesis and Crystal Structures of Substituted Benzenes and Benzoquinones as Tissue Factor VIIa Inhibitors

pp 4297–4312
Publication Date (Web): September 06, 2003 (Article)
DOI: 10.1021/jm030233b

The Combi-Targeting Concept:  Chemical Dissection of the Dual Targeting Properties of a Series of “Combi-Triazenes”

pp 4313–4321
Publication Date (Web): September 03, 2003 (Article)
DOI: 10.1021/jm030142e

SAR Analysis of Adenosine Diphosphate (Hydroxymethyl)pyrrolidinediol Inhibition of Poly(ADP-ribose) Glycohydrolase

pp 4322–4332
Publication Date (Web): August 29, 2003 (Article)
DOI: 10.1021/jm020541u

Imidazo[1,2-b]pyridazines, Novel Nucleus with Potent and Broad Spectrum Activity against Human Picornaviruses:  Design, Synthesis, and Biological Evaluation

pp 4333–4341
Publication Date (Web): August 21, 2003 (Article)
DOI: 10.1021/jm020583i

Structures and Cytotoxic Properties of Trichoverroids and Their Macrolide Analogues Produced by Saltwater Culture of Myrothecium verrucaria

pp 4342–4350
Publication Date (Web): August 23, 2003 (Article)
DOI: 10.1021/jm030090t

Metabolites of Febrifugine and Its Synthetic Analogue by Mouse Liver S9 and Their Antimalarial Activity against Plasmodium Malaria Parasite

pp 4351–4359
Publication Date (Web): August 29, 2003 (Article)
DOI: 10.1021/jm0302086

Brief Articles

Informative Library Design as an Efficient Strategy to Identify and Optimize Leads:  Application to Cyclin-Dependent Kinase 2 Antagonists

pp 4360–4364
Publication Date (Web): August 30, 2003 (Brief Article)
DOI: 10.1021/jm020472j