Journal of Medicinal Chemistry: Volume 46, Issue 1 (ACS Publications)

January 2, 2003

Volume 46, Issue 1

Pages 1-200

Letters

Specific Targeting of Acetylcholinesterase and Butyrylcholinesterase Recognition Sites. Rational Design of Novel, Selective, and Highly Potent Cholinesterase Inhibitors

Luisa Savini, Alessandra Gaeta, Caterina Fattorusso, Bruno Catalanotti, Giuseppe Campiani, Luisa Chiasserini, Cesare Pellerano, Ettore Novellino, Dawn McKissic, and Ashima Saxena

pp 1–4

Publication Date (Web): December 07, 2002 (Letter)

DOI: 10.1021/jm0255668

Abstract | Supporting Info

Hi-Res PDF[193K]

First X-ray Cocrystal Structure of a Bacterial FabH Condensing Enzyme and a Small Molecule Inhibitor Achieved Using Rational Design and Homology Modeling

Robert A. Daines, Israil Pendrak, Kelvin Sham, Glenn S. Van Aller, Alex K. Konstantinidis, John T. Lonsdale, Cheryl A. Janson, Xiayang Qiu, Martin Brandt, Sanjay S. Khandekar, Carol Silverman, and Martha S. Head

pp 5–8

Publication Date (Web): December 02, 2002 (Letter)

DOI: 10.1021/jm025571b

Abstract | Supporting Info

Hi-Res PDF[259K]

Structure−Activity Relationship of (1-Aryl-2-piperazinylethyl)piperazines: Antagonists for the AGRP/Melanocortin Receptor Binding

Premilla N. Arasasingham, Christopher Fotsch, Xiaohu Ouyang, Mark H. Norman, Michael G. Kelly, Kevin L. Stark, Bill Karbon, Clarence Hale, James W. Baumgartner, Martha Zambrano, Janet Cheetham, and Nuria A. Tamayo

pp 9–11

Publication Date (Web): November 27, 2002 (Letter)

DOI: 10.1021/jm0255522

Table of Contents

Letters

Specific Targeting of Acetylcholinesterase and Butyrylcholinesterase Recognition Sites. Rational Design of Novel, Selective, and Highly Potent Cholinesterase Inhibitors

First X-ray Cocrystal Structure of a Bacterial FabH Condensing Enzyme and a Small Molecule Inhibitor Achieved Using Rational Design and Homology Modeling

Structure−Activity Relationship of (1-Aryl-2-piperazinylethyl)piperazines: Antagonists for the AGRP/Melanocortin Receptor Binding

Stereoselective Synthesis of β-Lactams with Polyaromatic Imines: Entry to New and Novel Anticancer Agents

Articles

Desferrithiocin Analogue Based Hexacoordinate Iron(III) Chelators

Surface Descriptors for Protein−Ligand Affinity Prediction

The Power of Visual Imagery in Drug Design. Isopavines as a New Class of Morphinomimetics and Their Human Opioid Receptor Binding Activity

Synthesis and Structure−Activity Relationships of 6,7-Disubstituted 4-Anilinoquinoline-3-carbonitriles. The Design of an Orally Active, Irreversible Inhibitor of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor (EGFR) and the Human Epidermal Growth Factor Receptor-2 (HER-2)

Hydantoin-Substituted 4,6-Dichloroindole-2-carboxylic Acids as Ligands with High Affinity for the Glycine Binding Site of the NMDA Receptor

Homology Modeling of Rat and Human Cytochrome P450 2D (CYP2D) Isoforms and Computational Rationalization of Experimental Ligand-Binding Specificities

Unique Structure−Activity Relationship for 4-Isoxazolyl-1,4-dihydropyridines

Synthetic Analogues of the Bacterial Signal (Quorum Sensing) Molecule N-(3-Oxododecanoyl)-l-homoserine Lactone as Immune Modulators

Relationship between Stereochemistry and the β3-Adrenoceptor Agonistic Activity of 4‘-Hydroxynorephedrine Derivative as an Agent for Treatment of Frequent Urination and Urinary Incontinence

Discovery of a Thieno[2,3-d]pyrimidine-2,4-dione Bearing a p-Methoxyureidophenyl Moiety at the 6-Position: A Highly Potent and Orally Bioavailable Non-Peptide Antagonist for the Human Luteinizing Hormone-Releasing Hormone Receptor

Biphenylsulfonamide Endothelin Receptor Antagonists. 4. Discovery of N-[[2‘-[[(4,5-Dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1‘-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), A Highly Potent and Orally Active ETA Selective Antagonist

New Benzo[h][1,6]naphthyridine and Azepino[3,2-c]quinoline Derivatives as Selective Antagonists of 5-HT4 Receptors: Binding Profile and Pharmacological Characterization

Studies on the Mechanisms of Activation of Indolequinone Phosphoramidate Prodrugs

8-Aza-immucillins as Transition-State Analogue Inhibitors of Purine Nucleoside Phosphorylase and Nucleoside Hydrolases

New N-n-Propyl-Substituted 3-Aryl- and 3-Cyclohexylpiperidines as Partial Agonists at the D4 Dopamine Receptor

Structure−Activity Relationships of 1,2,4-Benzotriazine 1,4-Dioxides as Hypoxia-Selective Analogues of Tirapazamine

Synthesis and Antitumor Activity of Conjugates of Muramyldipeptide or Normuramyldipeptide with Hydroxyacridine/Acridone Derivatives

Brief Articles

Synthesis and in Vivo Antitumor Activity of Poly(l-glutamic acid) Conjugates of 20(S)-Camptothecin

Molecular Basis of the Antitumor Activities of 2-Crotonyloxymethyl-2-cycloalkenones

Discovery of a Novel and Highly Potent Noncompetitive AMPA Receptor Antagonist

Relationship between Stereochemistry and the β₃-Adrenoceptor Agonistic Activity of 4‘-Hydroxynorephedrine Derivative as an Agent for Treatment of Frequent Urination and Urinary Incontinence

Biphenylsulfonamide Endothelin Receptor Antagonists. 4. Discovery of N-[[2‘-[[(4,5-Dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1‘-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), A Highly Potent and Orally Active ET_A Selective Antagonist

New Benzo[h][1,6]naphthyridine and Azepino[3,2-c]quinoline Derivatives as Selective Antagonists of 5-HT₄ Receptors: Binding Profile and Pharmacological Characterization

New N-n-Propyl-Substituted 3-Aryl- and 3-Cyclohexylpiperidines as Partial Agonists at the D₄ Dopamine Receptor