三取代咪唑衍生物作为p38α丝裂原活化蛋白激酶抑制剂的合成及生物学评价
Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase.
作者信息
Kim Dae-Kee, Lim Jin-Hwi, Lee Jung A, Dewang Purushottam M
机构信息
College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-gu, Seoul 120-750, Korea.
出版信息
Bioorg Med Chem Lett. 2008 Jul 15;18(14):4006-10. doi: 10.1016/j.bmcl.2008.06.007. Epub 2008 Jun 6.
PMID:18571921
Abstract
A series of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH(2)-substituted benzyl moiety have been synthesized and evaluated for p38alpha MAP kinase inhibitory activity. Among them, compounds 22c, 27b, and 28b inhibited p38alpha MAP kinase with IC(50) values 27.6, 28, and 31 nM, respectively.
摘要
一系列含有4-氟苯基、嘧啶环以及氰基或氨甲酰基取代苄基部分的三取代咪唑衍生物已被合成，并对其p38α丝裂原活化蛋白激酶抑制活性进行了评估。其中，化合物22c、27b和28b对p38α丝裂原活化蛋白激酶具有抑制作用，其半数抑制浓度（IC50）值分别为27.6、28和31 nM。
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