2-Arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: Synthesis, binding studies and behavioral efficacy

Abstract 2-Arylamino-4-trifluoromethyl-5-aminomethylthiazoles represent a novel series of high-affinity corticotropin releasing factor-1 receptor (CRF 1 R) antagonists that are prepared in three steps in good overall yields. Herein, we report binding SAR as well as anxiolytic activity of an exemplary compound ( 7a , K i =8.6 nM) in a mouse canopy model.