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. 2010 Jun 15;20(12):3669-74.
doi: 10.1016/j.bmcl.2010.04.094. Epub 2010 Apr 24.

Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists

Dmitry Zuev  1 , Vivekananda M Vrudhula, Jodi A Michne, Bireshwar Dasgupta, Sokhom S Pin, Xiaohua Stella Huang, Dedong Wu, Qi Gao, Jie Zhang, Matthew T Taber, John E Macor, Gene M Dubowchik
Affiliations

Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists

Dmitry Zuev et al. Bioorg Med Chem Lett. .

Abstract

A novel series of [6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethyl]-dialkylamines was discovered as potent CRF(1)R antagonists. The optimization of binding affinity in the series by the parallel reaction approach is discussed herein.

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