2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists:: Synthesis, binding studies and behavioral efficacy

被引：17

作者：

Dubowchik, GM ^{[1
]}

Michne, JA ^{[1
]}

Zuev, D ^{[1
]}

Schwartz, W ^{[1
]}

Scola, PM ^{[1
]}

James, CA ^{[1
]}

Ruediger, EH ^{[1
]}

Pin, SS ^{[1
]}

Burris, KD ^{[1
]}

Balanda, LA ^{[1
]}

Gao, Q ^{[1
]}

Wu, DD ^{[1
]}

Fung, L ^{[1
]}

Fiedler, T ^{[1
]}

Browman, KE ^{[1
]}

Taber, MT ^{[1
]}

Zhang, J ^{[1
]}

机构：

[1] Bristol Myers Squibb Pharmaceut Res Inst, Wallingford, CT 06492 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 22期

关键词：

D O I：

10.1016/j.bmcl.2003.08.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-Arylamino-4-trifluoromethyl-5-aminomethylthiazoles represent a novel series of high-affinity corticotropin releasing factor-1 receptor (CRF1R) antagonists that are prepared in three steps in good overall yields. Herein, we report binding SAR as well as anxiolytic activity of an exemplary compound (7a, K-i = 8.6 nM) in a mouse canopy model. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：3997 / 4000

页数：4

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