Journal of Medicinal Chemistry: Volume 48, Issue 5 (ACS Publications)

March 10, 2005

Volume 48, Issue 5

Pages 1297-1684

About the Cover: Interaction of the β-L-enantiomer of a 4'-C-ethynyl-2',3'-dideoxynucleoside analogue (ent-14-TP) at the active site of HIV reverse transcriptase (Siddiqui, M. A.; et al. J. Med. Chem. 2004, 47, 5041-5048).

Perspective

New Approaches toward Anti-HIV Chemotherapy

Erik De Clercq

pp 1297–1313

Publication Date (Web): February 12, 2005 (Perspective)

DOI: 10.1021/jm040158k

Abstract

Hi-Res PDF[280K]

Letters

Development and Preliminary Optimization of Indole-N-Acetamide Inhibitors of Hepatitis C Virus NS5B Polymerase

Steven Harper, Barbara Pacini, Salvatore Avolio, Marcello Di Filippo, Giovanni Migliaccio, Ralph Laufer, Raffaele De Francesco, Michael Rowley, and Frank Narjes

pp 1314–1317

Publication Date (Web): February 8, 2005 (Letter)

DOI: 10.1021/jm049122i

Table of Contents

Perspective

New Approaches toward Anti-HIV Chemotherapy

Letters

Development and Preliminary Optimization of Indole-N-Acetamide Inhibitors of Hepatitis C Virus NS5B Polymerase

Identification of 2-(4-Benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an Orally Efficacious Melanin-Concentrating Hormone Receptor 1 Antagonist for the Treatment of Obesity

Articles

Synthesis of NO-Donor Bisphosphonates and Their in-Vitro Action on Bone Resorption

Solid-Phase Total Synthesis of Kahalalide A and Related Analogues

Synthesis and Biological Evaluation of Meperidine Analogues at Monoamine Transporters

Design, Synthesis, and in Vitro Evaluation of Dipeptide-Based Antibody Minor Groove Binder Conjugates

Novel Potent Orally Active Selective VEGFR-2 Tyrosine Kinase Inhibitors: Synthesis, Structure−Activity Relationships, and Antitumor Activities of N-Phenyl-N‘-{4-(4-quinolyloxy)phenyl}ureas

Discovery of Functionally Selective 7,8,9,10-Tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABAA Receptor Agonists at the α3 Subunit

Design and Synthesis of Melanocortin Peptides with Candidacidal and Anti-TNF-α Properties

Synthesis of Phosphonated Carbocyclic 2‘-Oxa-3‘-aza-nucleosides: Novel Inhibitors of Reverse Transcriptase

β-Lactam Screening by Specific Residues of the OmpF Eyelet

Synthesis and Biological Evaluation of Novel Naphthocarbazoles as Potential Anticancer Agents

Cationic Polysaccharides as Antiprion Agents

N- and C-Terminal Modifications of Nociceptin/Orphanin FQ Generate Highly Potent NOP Receptor Ligands

Nonpolar and Short Side Chain Groups at C-11β of Estradiol Result in Antiestrogens

CoMFA and CoMSIA Analyses of Pneumocystis carinii Dihydrofolate Reductase, Toxoplasma gondii Dihydrofolate Reductase, and Rat Liver Dihydrofolate Reductase

Design And Synthesis of a Novel Potent Myelin Basic Protein Epitope 87−99 Cyclic Analogue: Enhanced Stability and Biological Properties of Mimics Render Them a Potentially New Class of Immunomodulators

CHMIS-C: A Comprehensive Herbal Medicine Information System for Cancer

A Shape-Based 3-D Scaffold Hopping Method and Its Application to a Bacterial Protein−Protein Interaction

Dynamic Receptor-Based Pharmacophore Model Development and Its Application in Designing Novel HIV-1 Integrase Inhibitors

NMR Studies Reveal Structural Differences between the Gallium and Yttrium Complexes of DOTA-d-Phe1-Tyr3-octreotide

Novel Ligands for the Chemokine Receptor-3 (CCR3): A Receptor-Modeling Study Based on 5D-QSAR

Design and Biological Evaluation of Linear and Cyclic Phosphopeptide Ligands of the N-Terminal SH2 Domain of Protein Tyrosine Phosphatase SHP-1

Rational Design, Synthesis, and Structure−Activity Relationships of Aryltriazoles as Novel Corticotropin-Releasing Factor-1 Receptor Antagonists

Synthesis, Biological Evaluation, and Molecular Modeling of Ribose-Modified Adenosine Analogues as Adenosine Receptor Agonists

Synthesis and Evaluation of (Pyridylmethylene)tetrahydronaphthalenes/-indanes and Structurally Modified Derivatives: Potent and Selective Inhibitors of Aldosterone Synthase

Bisaryloxime Ethers as Potent Inhibitors of Transthyretin Amyloid Fibril Formation

Synthesis, Characterization, and Comparative in Vitro Cytotoxicity Studies of Platinum(II), Palladium(II), and Gold(III) Methylsarcosinedithiocarbamate Complexes

Structure-Based Design, Synthesis, and Study of Potent Inhibitors of β-Ketoacyl-acyl Carrier Protein Synthase III as Potential Antimicrobial Agents

Discovery and Evaluation of 2-Anilino-5-aryloxazoles as a Novel Class of VEGFR2 Kinase Inhibitors

3D-QSAR Comparative Molecular Field Analysis on Opioid Receptor Antagonists: Pooling Data from Different Studies

Force Field Design and Molecular Dynamics Simulations of the Carbapenem- and Cephamycin-Resistant Dinuclear Zinc Metallo-β-lactamase from Bacteroides fragilis and Its Complex with a Biphenyl Tetrazole Inhibitor

A General Method for Exploiting QSAR Models in Lead Optimization

Discovery of a Novel Class of Reversible Non-Peptide Caspase Inhibitors via a Structure-Based Approach

Searching for a Reliable Orientation of Ligands in Their Binding Site: Comparison between a Structure-Based (Glide) and a Ligand-Based (FIGO) Approach in the Case Study of PDE4 Inhibitors

Brief Articles

Structure of a Synthetic Fragment of the LALF Protein When Bound to Lipopolysaccharide

Copper(II) and Cobalt(III) Pyridoxal Thiosemicarbazone Complexes with Nitroprusside as Counterion: Syntheses, Electronic Properties, and Antileukemic Activity

Major Effect of Pyrrolic N-Benzylation in Norbinaltorphimine, the Selective κ-Opioid Receptor Antagonist

Identification of Small Molecule Chemical Inhibitors of the Collagen-Specific Chaperone Hsp47

Discovery of Functionally Selective 7,8,9,10-Tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA_A Receptor Agonists at the α₃ Subunit

NMR Studies Reveal Structural Differences between the Gallium and Yttrium Complexes of DOTA-d-Phe¹-Tyr³-octreotide