Phenoxypyrimidine inhibitors of p38α kinase:: Synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-2-phenoxypyrimidin-4-yl) imidazoles

被引:41
作者
Boehm, JC
Bower, MJ
Gallagher, TF
Kassis, S
Johnson, SR
Adams, JL
机构
[1] GlaxoSmithKline, Dept Med Chem, King Of Prussia, PA 19406 USA
[2] GlaxoSmithKline, Dept Cheminformat, King Of Prussia, PA 19406 USA
[3] GlaxoSmithKline, Dept Bone & Cartilage Biol, King Of Prussia, PA 19406 USA
[4] GlaxoSmithKline, Dept Phys & Struct Chem, King Of Prussia, PA 19406 USA
关键词
D O I
10.1016/S0960-894X(01)00163-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
As a continuation of our work with 1,4,5 substituted imidazole inhibitors of p38 alpha, we report a series of 1-(4-piperidinyl)-4-(4-fluorophenyl)-5-(2-phenoxy-4-pyrimidinyl) imidazoles related to 7. The componds have IC50's for inhibition of p38 alpha ranging from 6.0 to 650 nM. Statistical analysis of the p38 alpha inhibitor potencies shows a correlation of IC50's with the electron donating strength of low molecular weight substituents. (C) 2001 Elsevier Science Ltd. All rights reserved.
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页码:1123 / 1126
页数:4
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