咪唑并[1,2-a]苯并咪唑类作为促肾上腺皮质激素释放因子1受体拮抗剂的合成及构效关系
Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists.
作者信息
Han Xiaojun, Pin Sokhom S, Burris Kevin, Fung Lawrence K, Huang Stella, Taber Matthew T, Zhang Jie, Dubowchik Gene M
机构信息
Pharmaceutical Research Institute, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem Lett. 2005 Sep 15;15(18):4029-32. doi: 10.1016/j.bmcl.2005.06.028.
PMID:15982881
Abstract
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).
摘要
8-芳基-1,3a,8-三氮杂环戊并[a]茚类化合物代表了一类新型的具有高结合亲和力的促肾上腺皮质激素释放因子1受体拮抗剂。在此，我们报道了它们的合成方法、构效关系以及化合物8e（K(i)=23 nM）的药代动力学性质。
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