Synthesis, structure–activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists

7-Aryl-6,7-dihydroimidazoimidazoles represent a novel series of high-affinity corticotropin-releasing factor 1 receptor antagonists. Here, we report their synthesis and SAR as well as behavioral activity of two exemplary compounds, 7b and 7k, in a mouse canopy model of anxiety.

Graphical abstractThe synthesis and SAR of constrained dihydroimidazoimidazoles, and behavioral activity of compounds 7b (Ki 42 nM) and 7k (Ki 41 nM) in a mouse canopy model of anxiety, are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide