Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists |
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| Authors: | Huang Charles Q Grigoriadis Dimitri E Liu Zhengyu McCarthy James R Ramphal John Webb Thomas Whitten Jeffrey P Xie Michael Y Chen Chen |
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| Institution: | Neurocrine Biosciences, Inc, 10555 Science Centre Drive, San Diego, CA 92121, USA. chuang@neurocrine.com |
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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. |
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