Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor1 (CRF1) receptor antagonists
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.
Huang, Charles Q.,Grigoriadis, Dimitri E.,Liu, Zhengyu,McCarthy, James R.,Ramphal, John,Webb, Thomas,Whitten, Jeffrey P.,Xie, Michael Y.,Chen, Chen
p. 2083 - 2086
(2007/10/03)
CRF receptor antagonists and methods relating thereto
CRF receptor antagonists are disclosed. Such receptor antagonists are thiadiazole-, pyrimidine-, triazine-, and triazole-containing compounds substituted with both a C3-C14 monocyclic or fused, homoaryl or heteroaryl group and a substituted amine group. The CFR receptor antagonists have utility in the treatment of a variety of disorders, including disorders associated with the hypersecretion of CRF.
-
(2008/06/13)
More Articles about upstream products of 186342-55-2