Journal of Medicinal Chemistry: Volume 48, Issue 15 (ACS Publications)

July 28, 2005

Volume 48, Issue 15

Pages 4705-5058

About the Cover: Illustration of the binding mode of a biheteroaryl inhibitor to vascular endothelial growth factor receptor-2 (Kuo, G.-H.; et al. J. Med. Chem. 2005, 48, 1886-1900).

Perspective

Neuronal Nicotinic Acetylcholine Receptors: Structural Revelations, Target Identifications, and Therapeutic Inspirations

Anders A. Jensen, Bente Frølund, Tommy Liljefors, and Povl Krogsgaard-Larsen

pp 4705–4745

Publication Date (Web): July 21, 2005 (Perspective)

DOI: 10.1021/jm040219e

Abstract

Hi-Res PDF[2222K]

Letters

Biaryl Ureas as Potent and Orally Efficacious Melanin Concentrating Hormone Receptor 1 Antagonists for the Treatment of Obesity

Anandan Palani, Sherry Shapiro, Mark D. McBriar, John W. Clader, William J. Greenlee, Brian Spar, Timothy J. Kowalski, Constance Farley, John Cook, Margaret van Heek, Blair Weig, Kim O'Neill, Michael Graziano, and Brian Hawes

pp 4746–4749

Publication Date (Web): June 24, 2005 (Letter)

DOI: 10.1021/jm0503852

Table of Contents

Perspective

Neuronal Nicotinic Acetylcholine Receptors: Structural Revelations, Target Identifications, and Therapeutic Inspirations

Letters

Biaryl Ureas as Potent and Orally Efficacious Melanin Concentrating Hormone Receptor 1 Antagonists for the Treatment of Obesity

Rational Design of Non-Nucleoside, Potent, and Orally Bioavailable Adenosine Deaminase Inhibitors: Predicting Enzyme Conformational Change and Metabolism

Articles

Discovery of High-Affinity Ligands of σ1 Receptor, ERG2, and Emopamil Binding Protein by Pharmacophore Modeling and Virtual Screening

Neoclerodane Diterpenes as a Novel Scaffold for μ Opioid Receptor Ligands

Dicarboxylic Acid Azacycle l-Prolyl-pyrrolidine Amides as Prolyl Oligopeptidase Inhibitors and Three-Dimensional Quantitative Structure−Activity Relationship of the Enzyme−Inhibitor Interactions

Structural Analysis of Isoform-Specific Inhibitors Targeting the Tetrahydrobiopterin Binding Site of Human Nitric Oxide Synthases

Inhibitors of Trypanosoma cruzi Trypanothione Reductase Revealed by Virtual Screening and Parallel Synthesis

Synthesis and Mechanism of Action Studies of a Series of Norindenoisoquinoline Topoisomerase I Poisons Reveal an Inhibitor with a Flipped Orientation in the Ternary DNA−Enzyme−Inhibitor Complex As Determined by X-ray Crystallographic Analysis

Control of Protein−Protein Interactions: Structure-Based Discovery of Low Molecular Weight Inhibitors of the Interactions between Pin1 WW Domain and Phosphopeptides

Molecular Dynamics Simulations of the Endocannabinoid N-Arachidonoylethanolamine (Anandamide) in a Phospholipid Bilayer: Probing Structure and Dynamics

Carbonic Anhydrase Inhibitors. Design of Fluorescent Sulfonamides as Probes of Tumor-Associated Carbonic Anhydrase IX That Inhibit Isozyme IX-Mediated Acidification of Hypoxic Tumors

Combination of Molecular Modeling, Site-Directed Mutagenesis, and SAR Studies To Delineate the Binding Site of Pyridopyrimidine Antagonists on the Human CCK1 Receptor

Iterative Approach to the Discovery of Novel Degarelix Analogues: Substitutions at Positions 3, 7, and 8. Part II

Design, Synthesis, and Enzymatic Evaluation of N1-Acyloxyalkyl- and N1-Oxazolidin-2,4-dion-5-yl-Substituted β-lactams as Novel Inhibitors of Human Leukocyte Elastase

Structure-Based Design, Synthesis, and Biological Evaluation of Inhibitors of Mycobacterium tuberculosis Type II Dehydroquinase

Inclusion of a Photosensitizer in Liposomes Formed by DMPC/Gemini Surfactant: Correlation between Physicochemical and Biological Features of the Complexes

Synthesis and Structure−Activity Relationships of Pyrazine-Pyridine Biheteroaryls as Novel, Potent, and Selective Vascular Endothelial Growth Factor Receptor-2 Inhibitors

“Reversine” and Its 2-Substituted Adenine Derivatives as Potent and Selective A3 Adenosine Receptor Antagonists

Synthesis, Structure−Activity Relationships, and Biological Evaluation of Fatty Alcohol Phosphates as Lysophosphatidic Acid Receptor Ligands, Activators of PPARγ, and Inhibitors of Autotaxin

Synthesis and Structure−Activity Relationships of a New Series of Retinoid-Related Biphenyl-4-ylacrylic Acids Endowed with Antiproliferative and Proapoptotic Activity

Range and Sensitivity as Descriptors of Molecular Property Spaces in Dynamic QSAR Analyses

Spiro and Dispiro-1,2,4-trioxolanes as Antimalarial Peroxides: Charting a Workable Structure−Activity Relationship Using Simple Prototypes

Discovery of Novel Trisubstituted Asymmetric Derivatives of (2S,4R,5R)-2-benzhydryl-5-benzylaminotetrahydropyran-4-ol, Exhibiting High Affinity for Serotonin and Norepinephrine Transporters in a Stereospecific Manner

Synthesis and Radioligand Binding Studies of C-5- and C-8-Substituted 1-(3,4-Dimethoxybenzyl)-2,2-dimethyl-1,2,3,4-tetrahydroisoquinoliniums as SK Channel Blockers Related to N-Methyl-laudanosine and N-Methyl-noscapine

Antitumor Activity of C-Methyl-β-d-ribofuranosyladenine Nucleoside Ribonucleotide Reductase Inhibitors

3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-Dioxides as ATP-Sensitive Potassium Channel Openers: Effect of 6,7-Disubstitution on Potency and Tissue Selectivity

New 2-Arylpyrazolo[4,3-c]quinoline Derivatives as Potent and Selective Human A3 Adenosine Receptor Antagonists

Conformational Constraint in Oxazolidinone Antibacterials. Synthesis and Structure−Activity Studies of (Azabicyclo[3.1.0]hexylphenyl)oxazolidinones

Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Brief Articles

Peptidyl Vinyl Ester Derivatives: New Class of Selective Inhibitors of Proteasome Trypsin-Like Activity

5‘-Homoneplanocin A Inhibits Hepatitis B and Hepatitis C

A New Simple and High-Yield Synthesis of Suberoylanilide Hydroxamic Acid and Its Inhibitory Effect Alone or in Combination with Retinoids on Proliferation of Human Prostate Cancer Cells

Effect of a 6-Cyano Substituent in 14-Oxygenated N-Methylmorphinans on Opioid Receptor Binding and Antinociceptive Potency

Book Reviews

Studies in Natural Products Chemistry. Volume 30. Bioactive Natural Products (Part K) Edited by Atta-Ur-Rahman. Elsevier, Amsterdam, The Netherlands. 2005. xiv + 963 pp. 17 × 24.45 cm. ISBN 0-3444-518-54-1. $506.00.

Nitric Oxide Donors: For Pharmaceutical and Biological Applications Edited by Peng George Wang, Tingwei Bill Cai, and Naoyuki Taniguchi. Wiley-VCH Verlag GmbH & Co. KgaA, Weinheim, Germany. 2005. xxi + 390 pp. 17.5 × 25 cm. ISBN 3-527-31015-0. $185.00.

Using Mass Spectrometry for Drug Metabolism Studies Edited by Walter A. Korfmacher. CRC Press, Boca Raton, FL. 2005. xii + 370 pp. 24 × 16 cm. ISBN 0-8493-1963-3. $159.95.

Additions and Corrections

3-Aminopyrazole Inhibitors of CDK2/Cyclin A as Antitumor Agents. 2. Lead Optimization.

Discovery of High-Affinity Ligands of σ₁ Receptor, ERG2, and Emopamil Binding Protein by Pharmacophore Modeling and Virtual Screening

Design, Synthesis, and Enzymatic Evaluation of N¹-Acyloxyalkyl- and N¹-Oxazolidin-2,4-dion-5-yl-Substituted β-lactams as Novel Inhibitors of Human Leukocyte Elastase

“Reversine” and Its 2-Substituted Adenine Derivatives as Potent and Selective A₃ Adenosine Receptor Antagonists

New 2-Arylpyrazolo[4,3-c]quinoline Derivatives as Potent and Selective Human A₃ Adenosine Receptor Antagonists