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ID: ALA1136357
Journal: Bioorg Med Chem Lett
Title: 2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy.
Authors: Dubowchik GM, Michne JA, Zuev D, Schwartz W, Scola PM, James CA, Ruediger EH, Pin SS, Burris KD, Balanda LA, Gao Q, Wu D, Fung L, Fiedler T, Browman KE, Taber MT, Zhang J.
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.
CiteXplore: 14592493