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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- …

…, TF Gallagher, S Kassis, SR Johnson, JL Adams

文献索引:Boehm, Jeffrey C.; Bower, Michael J.; Gallagher, Timothy F.; Kassis, Shouki; Johnson, Stephen R.; Adams, Jerry L. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 9 p. 1123 - 1126

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被引用次数: 32

摘要

As a continuation of our work with 1, 4, 5 substituted imidazole inhibitors of p38α, we report a series of 1-(4-piperidinyl)-4-(4-fluorophenyl)-5-(2-phenoxy-4-pyrimidinyl) imidazoles related to 7. The compounds have IC50's for inhibition of p38α ranging from 6.0 to 650nM. Statistical analysis of the p38α inhibitor potencies shows a correlation of IC50's with the electron donating strength of low molecular weight substituents.