2-二烷基氨基-4-芳基嘧啶作为强效和选择性促肾上腺皮质激素释放因子(1)(CRF(1))受体拮抗剂的设计、合成及构效关系研究
Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists.
作者信息
Huang Charles Q, Grigoriadis Dimitri E, Liu Zhengyu, McCarthy James R, Ramphal John, Webb Thomas, Whitten Jeffrey P, Xie Michael Y, Chen Chen
机构信息
Neurocrine Biosciences, Inc, 10555 Science Centre Drive, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2004 May 3;14(9):2083-6. doi: 10.1016/j.bmcl.2004.02.053.
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.
设计并合成了一系列2-二烷基氨基-4-苯基嘧啶（7）作为促肾上腺皮质激素释放因子（CRF）（1）拮抗剂。对该系列进行的构效关系研究发现了强效且具选择性的拮抗剂7b和7n，它们带有一个4-（2,4,6-三取代苯基）环和一个庞大的2-（N-双（环丙烷）甲基-N-丙基）氨基基团。
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