Bioorganic & Medicinal Chemistry Letters 2004-05-03

Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists.

Charles Q Huang, Dimitri E Grigoriadis, Zhengyu Liu, James R McCarthy, John Ramphal, Thomas Webb, Jeffrey P Whitten, Michael Y Xie, Chen Chen

Index: Bioorg. Med. Chem. Lett. 14 , 2083-2086, (2004)

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Abstract

A series of 2-dialkylamino-4-phenylpyrimidines (7) was designed and synthesized as CRF(1) antagonists. SAR studies of this series resulted in the discovery of potent and selective antagonists 7b and 7n bearing a 4-(2,4,6-trisubstituted-phenyl) ring and a bulky 2-(N-bis(cyclopropane)methyl-N-propyl)amino group.