Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists

被引:41
作者
Han, XJ [1 ]
Pin, SS [1 ]
Burris, K [1 ]
Fung, LK [1 ]
Huang, S [1 ]
Taber, MT [1 ]
Zhang, J [1 ]
Dubowchik, GM [1 ]
机构
[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA
关键词
corticotropin-releasing factor 1; antagonists; SAR; pharmacokinetic properties;
D O I
10.1016/j.bmcl.2005.06.028
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
8-Aryl-1,3a,8-triaza-cyclopenta[a]indenes represent a novel series of high binding affinity corticotropin-releasing factor 1 receptor antagonists. Here, we report their synthesis, SAR, and pharmacokinetic properties of compound 8e (K-i = 23 nM). (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4029 / 4032
页数:4
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