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

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 (Ki = 23 nM).

Graphical abstractThe synthesis and SAR of imidazo[1,2-a]benzimidazoles and pharmacokinetic properties of compound 8e (Ki = 23 nM) are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide