Journal of Medicinal Chemistry: Volume 46, Issue 14 (ACS Publications)

July 3, 2003

Volume 46, Issue 14

Pages 2795-3180

About the Cover: Connolly surface map of the X-ray structure of the α-thrombin-cyclopentenedicarboxylic acid derivative complex (yellow) at 1.9 Å resolution superimposed on the X-ray structure of the α-thrombin-PPACK complex (magenta) (Thorstensson, F.; et al. J. Med. Chem. 2003, 46, 1165-1179).

Perspective

Higher-End Serotonin Receptors: 5-HT₅, 5-HT₆, and 5-HT₇

Richard A. Glennon

pp 2795–2812

Publication Date (Web): June 11, 2003 (Perspective)

DOI: 10.1021/jm030030n

Table of Contents

Perspective

Higher-End Serotonin Receptors: 5-HT5, 5-HT6, and 5-HT7

Letters

Design, Synthesis, and Evaluation of Novel Boronic-Chalcone Derivatives as Antitumor Agents

Dihydrofolate Reductase Mutant with Exceptional Resistance to Methotrexate but Not to Trimetrexate

4-Aryl-3-(hydroxyalkyl)quinolin-2-ones: Novel Maxi-K Channel Opening Relaxants of Corporal Smooth Muscle Targeted for Erectile Dysfunction

Articles

Synthesis of 1-Boraadamantaneamine Derivatives with Selective Astrocyte vs C6 Glioma Antiproliferative Activity. A Novel Class of Anti-Hepatitis C Agents with Potential to Bind CD81

Docking and Database Screening Reveal New Classes of Plasmodium falciparum Dihydrofolate Reductase Inhibitors

Simplified Discodermolide Analogues: Synthesis and Biological Evaluation of 4-epi-7-Dehydroxy-14,16-didemethyl-(+)-discodermolides as Microtubule-Stabilizing Agents

Synthesis and Evaluation of 17α-20E-21-(4-Substituted phenyl)-19-norpregna-1,3,5(10),20-tetraene-3,17β-diols as Probes for the Estrogen Receptor α Hormone Binding Domain

New Pyrimido[5,4-b]indoles as Ligands for α1-Adrenoceptor Subtypes

Information Decay in Molecular Docking Screens against Holo, Apo, and Modeled Conformations of Enzymes

Structure−Activity Relationship Comparison of (S)-2β-Substituted 3α-(Bis[4-fluorophenyl]methoxy)tropanes and (R)-2β-Substituted 3β-(3,4-Dichlorophenyl)tropanes at the Dopamine Transporter

Development of Natural Product-Derived Receptor Tyrosine Kinase Inhibitors Based on Conservation of Protein Domain Fold

A Quantitative Structure−Activity Relationship and Pharmacophore Modeling Investigation of Aryl-X and Heterocyclic Bisphosphonates as Bone Resorption Agents

Estrogen Receptor Modulators: Identification and Structure−Activity Relationships of Potent ERα-Selective Tetrahydroisoquinoline Ligands

Design, Synthesis, and Evaluation of Psorospermin/Quinobenzoxazine Hybrids as Structurally Novel Antitumor Agents

Dual Protein Farnesyltransferase−Geranylgeranyltransferase-I Inhibitors as Potential Cancer Chemotherapeutic Agents

A Convergent Approach to Cryptophycin 52 Analogues: Synthesis and Biological Evaluation of a Novel Series of Fragment A Epoxides and Chlorohydrins

Histamine-Releasing Activity and Binding to the FcεRIα Human Mast Cell Receptor Subunit of Mast Cell Degranulating Peptide Analogues with Alanine Substitutions

Development and Validation of k-Nearest-Neighbor QSPR Models of Metabolic Stability of Drug Candidates

Studies on the Synthesis and Biological Properties of Non-Carrier-Added [125I and 131I]-Labeled Arylalkylidenebisphosphonates: Potent Bone-Seekers for Diagnosis and Therapy of Malignant Osseous Lesions

Novel Selective Hindlimb Vasodilators: Synthesis and Biological Activity of 1-Acyl-4-aminopiperidine Derivatives

Nuclear Hormone Receptor Targeted Virtual Screening

Novel Potent 5-HT1F Receptor Agonists: Structure−Activity Studies of a Series of Substituted N-[3-(1-Methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides

Structure−Activity Relationships and Mechanism of Action of Antitumor Benzo[b]pyrano[3,2-h]acridin-7-one Acronycine Analogues

Design and Synthesis of 4,6-Di-tert-butyl-2,3-dihydro-5-benzofuranols as a Novel Series of Antiatherogenic Antioxidants

Bioactive Peptidic Analogues and Cyclostereoisomers of the Minimal Antinociceptive Histogranin Fragment-(7−10)

Synthesis and Anticonvulsant Activity of Novel Bicyclic Acidic Amino Acids

Design, Synthesis, and Biological Properties of New Bis(acridine-4-carboxamides) as Anticancer Agents

N-(3-Acyloxy-2-benzylpropyl)-N‘-[4-(methylsulfonylamino)benzyl]thiourea Analogues: Novel Potent and High Affinity Antagonists and Partial Antagonists of the Vanilloid Receptor

Identification of (3R)-7-Hydroxy-N-((1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a Novel Potent and Selective Opioid κ Receptor Antagonist

Design and Synthesis of Poly ADP-ribose Polymerase-1 Inhibitors. 2. Biological Evaluation of Aza-5[H]-phenanthridin-6-ones as Potent, Aqueous-Soluble Compounds for the Treatment of Ischemic Injuries

Structural Determinants of Selective Thyromimetics

Brief Articles

A Selective Human H4-Receptor Agonist: (−)-2-Cyano-1-methyl-3-{(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-yl}methylguanidine

Carbon Isosteres of the 4-Aminopyridine Substructure of Chloroquine: Effects on pKa, Hematin Binding, Inhibition of Hemozoin Formation, and Parasite Growth

A New Biotin Derivative−DOTA Conjugate as a Candidate for Pretargeted Diagnosis and Therapy of Tumors

Opioid Binding and in Vitro Profiles of a Series of 4-Hydroxy-3-methoxyindolomorphinans. Transformation of a δ-Selective Ligand into a High Affinity κ-Selective Ligand by Introduction of a 5,14-Substituted Bridge

Book Reviews

Cardiovascular Pharmacotherapeutics. Second Edition Edited by William H. Frishman, Edmund H. Sonnenblick, and Domenic A. Sica. McGraw-Hill Medical Publishing Division, New York. 2003. xxiv + 1072 pp. 22.5 × 29 cm. ISBN 0-07-136981-3. $159.00.

Modern Methods of Drug Discovery Edited by Alexander Hillisch and Rolf Hilgenfeld. Birkhäuser Verlag, Basel, Switzerland. viii + 292 pp. 17 × 24 cm. ISBN 3-7643-6081-X. 127.00 euro.

Additions and Corrections

Novel Dual Inhibitors of AChE and MAO Derived from Hydroxy Aminoindan and Phenethylamine as Potential Treatment for Alzheimer's Disease.

Higher-End Serotonin Receptors: 5-HT₅, 5-HT₆, and 5-HT₇

New Pyrimido[5,4-b]indoles as Ligands for α₁-Adrenoceptor Subtypes

Studies on the Synthesis and Biological Properties of Non-Carrier-Added [¹²⁵I and ¹³¹I]-Labeled Arylalkylidenebisphosphonates: Potent Bone-Seekers for Diagnosis and Therapy of Malignant Osseous Lesions

Novel Potent 5-HT_1F Receptor Agonists: Structure−Activity Studies of a Series of Substituted N-[3-(1-Methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides

A Selective Human H₄-Receptor Agonist: (−)-2-Cyano-1-methyl-3-{(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-yl}methylguanidine

Carbon Isosteres of the 4-Aminopyridine Substructure of Chloroquine: Effects on pK_a, Hematin Binding, Inhibition of Hemozoin Formation, and Parasite Growth