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. 2003 Nov 17;13(22):3997-4000.
doi: 10.1016/j.bmcl.2003.08.055.

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

Gene M Dubowchik  1 , Jodi A Michne, Dmitry Zuev, Wendy Schwartz, Paul M Scola, Clint A James, Edward H Ruediger, Sokhom S Pin, Kevin D Burris, Lynn A Balanda, Qi Gao, Dedong Wu, Lawrence Fung, Tracey Fiedler, Kaitlin E Browman, Matthew T Taber, Jie Zhang
Affiliations

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

Gene M Dubowchik et al. Bioorg Med Chem Lett. .

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.

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