Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists

被引：23
|
作者：
Huang, CQ
Wilcoxen, K
McCarthy, JR
Haddach, M
Webb, TR
Gu, J
Xie, YF
Grigoriadis, DE
Chen, C
机构：
[1] Neurocrine Biosci Inc, Dept Med Chem, San Diego, CA 92121 USA
[2] Neurocrine Biosci Inc, Dept Pharmacol, San Diego, CA 92121 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 19期
关键词：
D O I：
10.1016/S0960-894X(03)00684-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 4-substituted 8-aryl-2-methylquinolines 4 was designed and synthesized as highly potent antagonists for the human CRF1 receptor. This series of compounds displayed parallel SAR to other bicyclic systems such as pyrazolo[l,5-a]pyrimidines, with several compounds possessing low nanomolar binding affinity. In addition to the high potency, the basicity of this 4-aminoquinoline core may offer CRF1 antagonists with lower lipophilicity. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3375 / 3379
页数：5
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