Journal of Medicinal Chemistry: Volume 45, Issue 19 (ACS Publications)

September 12, 2002

Volume 45, Issue 19

Pages 4057-4378

About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy- 2-propenamide, bound to the catalytic core of histone deacetylase (Mai, A.; et al. J. Med. Chem. 2002, 45, 1778-1784). View the article.

Perspectives

Purine and Pyrimidine (P2) Receptors as Drug Targets

Kenneth A. Jacobson, Michael F. Jarvis, and Michael Williams

pp 4057–4093

Publication Date (Web): August 20, 2002 (Perspective)

DOI: 10.1021/jm020046y

Table of Contents

Perspectives

Purine and Pyrimidine (P2) Receptors as Drug Targets

Pyrimidinylpyrroloquinolones as Highly Potent and Selective PDE5 Inhibitors for Treatment of Erectile Dysfunction

Articles

Mazindol Analogues as Potential Inhibitors of the Cocaine Binding Site at the Dopamine Transporter

Benzo- and Cyclohexanomazindol Analogues as Potential Inhibitors of the Cocaine Binding Site at the Dopamine Transporter

Three-Dimensional Quantitative Structure−Activity Relationships of Mazindol Analogues at the Dopamine Transporter

Synthesis and Molecular Modeling of New 1-Aryl-3-[4-arylpiperazin-1-yl]-1-propane Derivatives with High Affinity at the Serotonin Transporter and at 5-HT1A Receptors

Molecular Modeling of the Interactions of Glutamate Carboxypeptidase II with Its Potent NAAG-Based Inhibitors

DrugScore Meets CoMFA: Adaptation of Fields for Molecular Comparison (AFMoC) or How to Tailor Knowledge-Based Pair-Potentials to a Particular Protein

6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-Dioxide Derivatives Potently and Selectively Activate ATP Sensitive Potassium Channels of Pancreatic β-Cells

Refinement and Evaluation of a Pharmacophore Model for Flavone Derivatives Binding to the Benzodiazepine Site of the GABAA Receptor

Azapeptides Structurally Based upon Inhibitory Sites of Cystatins as Potent and Selective Inhibitors of Cysteine Proteases

Synthesis of a Novel Series of Benzocycloalkene Derivatives as Melatonin Receptor Agonists

Synthesis of a Novel Series of Tricyclic Indan Derivatives as Melatonin Receptor Agonists

Selective Agonists at Group II Metabotropic Glutamate Receptors: Synthesis, Stereochemistry, and Molecular Pharmacology of (S)- and (R)-2-Amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric Acid

Novel Antibiotics for the Treatment of Gram-Positive Bacterial Infections

Acyclic Nucleoside Analogues as Novel Inhibitors of Human Mitochondrial Thymidine Kinase

N-[(2-Sulfo)-9-fluorenylmethoxycarbonyl]3-gentamicin C1 Is a Long-Acting Prodrug Derivative

Anti-AIDS Agents 49.1 Synthesis, Anti-HIV, and Anti-Fusion Activities of IC9564 Analogues Based on Betulinic Acid

Synthesis of New Molecular Probes for Investigation of Steroid Biosynthesis Induced by Selective Interaction with Peripheral Type Benzodiazepine Receptors (PBR)

Novel Structures Derived from 2-[[(2-Pyridyl)methyl]thio]-1H-benzimidazole as Anti-Helicobacter pylori Agents, Part 1

Novel Structures Derived from 2-[[(2-Pyridyl)methyl]thio]-1H-benzimidazole as Anti-Helicobacter pylori Agents, Part 2

2-Substituted 4-(Thio)chromenone 6-O-Sulfamates: Potent Inhibitors of Human Steroid Sulfatase

Structure−Activity Relationships of the Antimalarial Agent Artemisinin. 7. Direct Modification of (+)-Artemisinin and In Vivo Antimalarial Screening of New, Potential Preclinical Antimalarial Candidates

Monoclonal Antibody Conjugates of Doxorubicin Prepared with Branched Peptide Linkers: Inhibition of Aggregation by Methoxytriethyleneglycol Chains

Lysergamides of Isomeric 2,4-Dimethylazetidines Map the Binding Orientation of the Diethylamide Moiety in the Potent Hallucinogenic Agent N,N-Diethyllysergamide (LSD)

Do Structurally Similar Molecules Have Similar Biological Activity?

Inhibition of the Antibacterial Target UDP-(3-O-acyl)-N-acetylglucosamine Deacetylase (LpxC): Isoxazoline Zinc Amidase Inhibitors Bearing Diverse Metal Binding Groups

Brief Articles

Piperidine Analogues of 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): High Affinity Ligands for the Dopamine Transporter

Book Reviews

Mass Spectrometry in Drug Discovery Edited by David T. Rossi and Michael W. Sinz. Marcel Dekker, Inc., New York. 2002. viii + 420 pp. 16 × 23.5 cm. ISBN 0-8247-0607-2. $165.00.

Structure and Bonding By Jack Barrett. Wiley-Interscience and Royal Society of Chemistry, New York. 2002. vi + 181 pp. 19 × 24.5 cm. ISBN 0-471-22479-0. $34.95 (Paperback).

Peptide Antibiotics. Discovery, Modes of Action, and Applications Edited by Christopher J. Dutton, Mark A. Haxell, Hamish A. I. McArthur, and Richard G. Wax. Marcel Dekker, Inc., New York. 2002. viii + 296 pp. 16 × 23.5 cm. ISBN 0-8247-0245-X. $150.00

Pharmaceutical Chemistry. Therapeutic Aspects of Biomacromolecules By Christine M. Bladon. John Wiley & Sons, Inc., Chichester, West Sussex, U.K. 2002. xii + 221 pp. 17 × 24.5 cm. ISBN 0-4714-9637-5. $35.00.

Additions and Corrections

Synthesis and Biological Evaluation of 2-Substituted 3β-Tolyltropane Derivatives at Dopamine, Serotonin, and Norepinephrine Transporters.

Synthesis and Molecular Modeling of New 1-Aryl-3-[4-arylpiperazin-1-yl]-1-propane Derivatives with High Affinity at the Serotonin Transporter and at 5-HT_1A Receptors

Refinement and Evaluation of a Pharmacophore Model for Flavone Derivatives Binding to the Benzodiazepine Site of the GABA_A Receptor

N-[(2-Sulfo)-9-fluorenylmethoxycarbonyl]₃-gentamicin C₁ Is a Long-Acting Prodrug Derivative

Anti-AIDS Agents 49.¹ Synthesis, Anti-HIV, and Anti-Fusion Activities of IC9564 Analogues Based on Betulinic Acid