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

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

Bioorganic & Medicinal Chemistry Letters（2004）

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摘要

2-Arylamino-4-trifluoromethyl-5-aminomethylthiazoles represent a novel series of high-affinity corticotropin releasing factor-1 receptor (CRF1R) 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, Ki=8.6 nM) in a mouse canopy model.

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