Journal of Medicinal Chemistry: Volume 47, Issue 24 (ACS Publications)

November 18, 2004

Volume 47, Issue 24

Pages 5821-6112

About the Cover: Ribbon rendered illustration of the nuclear receptor heterodimer RXRα(cyan):PPARRγ (red) ligand binding domains bound with coactivator peptides (magenta) and agonist ligands (space-filling atoms where green is carbon, red is oxygen, and blue is nitrogen) (Haffner, C. D.; et al. J. Med. Chem. 2004, 47, 2010-2029).

Letters

Piperidine-Based Nocaine/Modafinil Hybrid Ligands as Highly Potent Monoamine Transporter Inhibitors: Efficient Drug Discovery by Rational Lead Hybridization

Jia Zhou, Rong He, Kenneth M. Johnson, Yanping Ye, and Alan P. Kozikowski

pp 5821–5824

Publication Date (Web): October 15, 2004 (Letter)

DOI: 10.1021/jm040117o

Table of Contents

Letters

Piperidine-Based Nocaine/Modafinil Hybrid Ligands as Highly Potent Monoamine Transporter Inhibitors: Efficient Drug Discovery by Rational Lead Hybridization

Discovery of Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 5 from a Series of N-(1,3-Diphenyl-1H- pyrazol-5-yl)benzamides That Potentiate Receptor Function in Vivo

An Orally Bioavailable, Functionally Selective Inverse Agonist at the Benzodiazepine Site of GABAA α5 Receptors with Cognition Enhancing Properties

Novel Purine Nitrile Derived Inhibitors of the Cysteine Protease Cathepsin K

Articles

Development of Cobalt(3,4-diarylsalen) Complexes as Tumor Therapeutics

A Novel Site-Directed Affinity Reagent for Cross-Linking Human Hemoglobin: Bis[2-(4-phosphonooxyphenoxy)carbonylethyl]phosphinic Acid

Fluorinated Phenylcyclopropylamines. 2. Effects of Aromatic Ring Substitution and of Absolute Configuration on Inhibition of Microbial Tyramine Oxidase

Pyrazolo[1,5-a]pyrimidines: Estrogen Receptor Ligands Possessing Estrogen Receptor β Antagonist Activity

Synthesis and Biological Evaluation of 1-Aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one Inhibitors of Cyclin-Dependent Kinases

Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.

Design of Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 2.

Synthesis of C2−C3‘N-Linked Macrocyclic Taxoids. Novel Docetaxel Analogues with High Tubulin Activity

Design, Synthesis, and Biological Evaluation of Conformationally Restricted Rivastigmine Analogues

Improved Structure−Activity Relationship Analysis of HIV-1 Protease Inhibitors Using Interaction Kinetic Data

Tetrahydrobiopterin Binding to Aromatic Amino Acid Hydroxylases. Ligand Recognition and Specificity

5-Substituted Tetrazoles as Bioisosteres of Carboxylic Acids. Bioisosterism and Mechanistic Studies on Glutathione Reductase Inhibitors as Antimalarials

Building Predictive Models for Protein Tyrosine Phosphatase 1B Inhibitors Based on Discriminating Structural Features by Reassembling Medicinal Chemistry Building Blocks

Design, Synthesis, and Biological Evaluation of the First Selective Nonpeptide AT2 Receptor Agonist

AT2-Selective Angiotensin II Analogues Containing Tyrosine-Functionalized 5,5-Bicyclic Thiazabicycloalkane Dipeptide Mimetics

Highly Potent 1-Aminocyclohexane-1-Carboxylic Acid Substituted V2 Agonists of Arginine Vasopressin

Centrally Acting and Metabolically Stable Thyrotropin-Releasing Hormone Analogues by Replacement of Histidine with Substituted Pyridinium

β-Oxygenated Analogues of the 5-HT2A Serotonin Receptor Agonist 1-(4-Bromo-2,5-dimethoxyphenyl)-2-aminopropane

Quantitative Structure−Activity Relationship of Sesquiterpene Lactones as Inhibitors of the Transcription Factor NF-κB

N1-Substituent Effects in the Selective Delivery of Polyamine Conjugates into Cells Containing Active Polyamine Transporters

Design, Synthesis, and Preliminary Pharmacological Evaluation of 4-Aminopiperidine Derivatives as N-Type Calcium Channel Blockers Active on Pain and Neuropathic Pain

Long Hydrocarbon Chain Keto Diols and Diacids that Favorably Alter Lipid Disorders in Vivo

Brief Articles

Synthesis of N3,5‘-Cyclo-4-(β-d-ribofuranosyl)-vic-triazolo[4,5-b]pyridin-5-one, a Novel Compound with Anti-Hepatitis C Virus Activity

Influence of Molecular Flexibility and Polar Surface Area Metrics on Oral Bioavailability in the Rat

A New Class of Acyclic 2-Alkyl-1,1,2-Triaryl (Z)-Olefins as Selective Cyclooxygenase-2 Inhibitors

Book Reviews

Contemporary Drug Synthesis By Jie-Jack Li, Douglas S. Johnson, Drago R. Sliskovic, and Bruce D. Roth. John Wiley & Sons, Inc., Hoboken, NJ. 2004. xv + 221 pp. 19.5 × 24.5 cm. ISBN 0-471-21480-9. $89.95.

A Handbook of Bioanalysis and Drug Metabo-lism Edited by Gary Evans. CRC Press, Boca Raton, FL. 2004. xvi + 390 pp. 18.5 × 26 cm. ISBN 0-415-27519-9. $129.95

An Orally Bioavailable, Functionally Selective Inverse Agonist at the Benzodiazepine Site of GABA_A α5 Receptors with Cognition Enhancing Properties

Design, Synthesis, and Biological Evaluation of the First Selective Nonpeptide AT₂ Receptor Agonist

AT₂-Selective Angiotensin II Analogues Containing Tyrosine-Functionalized 5,5-Bicyclic Thiazabicycloalkane Dipeptide Mimetics

Highly Potent 1-Aminocyclohexane-1-Carboxylic Acid Substituted V₂ Agonists of Arginine Vasopressin

β-Oxygenated Analogues of the 5-HT_2A Serotonin Receptor Agonist 1-(4-Bromo-2,5-dimethoxyphenyl)-2-aminopropane

N¹-Substituent Effects in the Selective Delivery of Polyamine Conjugates into Cells Containing Active Polyamine Transporters

Synthesis of N³,5‘-Cyclo-4-(β-d-ribofuranosyl)-vic-triazolo[4,5-b]pyridin-5-one, a Novel Compound with Anti-Hepatitis C Virus Activity