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ID: ALA1147540

Journal: Bioorg Med Chem Lett

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

Authors: Huang CQ, Grigoriadis DE, Liu Z, McCarthy JR, Ramphal J, Webb T, Whitten JP, Xie MY, Chen C.

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.

CiteXplore: 15080983

DOI: 10.1016/j.bmcl.2004.02.053