Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands

被引：16

作者：

Arvanitis, AG ^{[1
]}

Rescinito, JT

Arnold, CR

Wilde, RG

Cain, GA

Sun, JH

Yan, JS

Teleha, CA

Fitzgerald, LW

McElroy, J

Zaczek, R

Hartig, PR

Grossman, S

Arneric, SP

Gilligan, PJ

Olson, RE

Robertson, DW

机构：

[1] Bristol Myers Squibb Co, Expt Stn, Discovery Chem Wilmington, Wilmington, DE 19880 USA

[2] Bristol Myers Squibb Co, Expt Stn, CNS Dis Res, Wilmington, DE 19880 USA

[3] Bristol Myers Squibb Co, Expt Stn, Drug Metab & Pharmacokinet, Wilmington, DE 19880 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(02)00833-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of high affinity CRF receptor ligands with an imidazo[4,5-b]pyridine core is described. Individual analogues were synthesized and tested in a rat CRF receptor binding assay. The best compounds were further tested in the dog N-in-1 pharmaco-kinetic model to assess plasma levels at 1 mg/kg (po) and in the rat situational anxiety model to assess anxiolytic efficacy at 3 mg/kg (po). The structure-activity relationships for good receptor binding affinity are described herein. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：125 / 128

页数：4

共 13 条

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