Phenoxypyrimidine inhibitors of p38 alpha 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

Citation
Jc. Boehm et al., Phenoxypyrimidine inhibitors of p38 alpha 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, BIOORG MED, 11(9), 2001, pp. 1123-1126
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
9
Year of publication
2001
Pages
1123 - 1126
Database
ISI
SICI code
0960-894X(20010507)11:9<1123:PIOPAK>2.0.ZU;2-V
Abstract
As a continuation of our work with 1,4,5 substituted imidazole inhibitors o f 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 analysi s of the p38 alpha inhibitor potencies shows a correlation of IC50's with t he electron donating strength of low molecular weight substituents. (C) 200 1 Elsevier Science Ltd. All rights reserved.