Bioorganic & Medicinal Chemistry Letters 2010-06-15

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, 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

Index: Bioorg. Med. Chem. Lett. 20 , 3669-3674, (2010)

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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.Copyright 2010 Elsevier Ltd. All rights reserved.