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.

Related Compounds

  • 2-Pipecoline

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