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

…, DE Grigoriadis, Z Liu, JR McCarthy, J Ramphal…

Index: Huang, Charles Q.; Grigoriadis, Dimitri E.; Liu, Zhengyu; McCarthy, James R.; Ramphal, John; Webb, Thomas; Whitten, Jeffrey P.; Xie, Michael Y.; Chen, Chen Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 9 p. 2083 - 2086

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Citation Number: 12

Abstract

A series of 2-dialkylamino-4-phenylpyrimidines (7) was designed and synthesized as CRF1 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.