Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-α]pyrimidines as potent CRF1 receptor antagonists

被引：36

作者：

Huang, CQ

Wilcoxen, KM

Grigoriadis, DE

McCarthy, JR

Chen, C

机构：

[1] Neurocrine Biosci Inc, Dept Med Chem, San Diego, CA 92129 USA

[2] Neurocrine Biosci Inc, Dept Pharmacol, San Diego, CA 92129 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 15期

关键词：

D O I：

10.1016/j.bmcl.2004.05.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines was designed and synthesized as antagonists for the corticotrophinreleasing factor-1 (CRF1) receptor. Several compounds such as 20c (K-i = 10nM) exhibited good binding affinities at the CRF1 receptor. In addition, 20c had adequate solubility in water. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：3943 / 3947

页数：5

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