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2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: Synthesis, binding studies and behavioral efficacy
2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: Synthesis, binding studies and behavioral efficacy BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Dubowchik, G. M., Michne, J. A., Zuev, D., Schwartz, W., Scola, P. M., James, C. A., Ruediger, E. H., Pin, S. S., Burris, K. D., Balanda, L. A., Gao, Q., Wu, D. D., Fung, L., Fiedler, T., Browman, K. E., Taber, M. T., Zhang, J. 2003; 13 (22): 3997-4000Abstract
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.
View details for DOI 10.1016/j.bmcl.2003.08.055
View details for Web of Science ID 000186486400024
View details for PubMedID 14592493