Substituted tetraazaacenaphthylenes as potent CRF1 receptor antagonists for the treatment of depression and anxiety

被引：7

作者：

St-Denis, Y

Di Fabio, R

Bernasconi, G

Castiglioni, E

Contini, S

Donati, D

Fazzolari, E

Gentile, G

Ghirlanda, D

Marchionni, C

Messina, F

Micheli, F

Pavone, F

Pasquarello, A

Sabbatini, FM

Zampori, MG

Arban, R

Vitulli, G

机构：

[1] GlaxoSmithKline Med Res Ctr, Dept Med Chem, I-37135 Verona, Italy

[2] GlaxoSmithKline Med Res Ctr, Dept Pharmacol, I-37135 Verona, Italy

[3] GlaxoSmithKline Med Res Ctr, Dept Drug Metab & Pharmacokinet, I-37135 Verona, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 16期

关键词：

D O I：

10.1016/j.bmcl.2005.05.040

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two isomers of the hexahydro-tetraazaacenaphthylene templates (1 and 2) are presented as novel, potent, and selective corticotropin releasing factor-1 (CRF1) receptor antagonists. In this paper, we report the affinity and SAR of a series of compounds, as well as pharmacokinetic characterization of a chosen set. The anxiolitic activity of a selected example (2ba) in the rat pup vocalization model is also presented. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：3713 / 3716

页数：4

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