Phenoxypyrimidine inhibitors of p38alpha 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 Chem Lett. 2001 May 7;11(9):1123-6. doi: 10.1016/s0960-894x(01)00163-9.


As a continuation of our work with 1,4,5 substituted imidazole inhibitors of p38alpha, 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 p38alpha ranging from 6.0 to 650nM. Statistical analysis of the p38beta inhibitor potencies shows a correlation of IC50's with the electron donating strength of low molecular weight substituents.

MeSH terms

  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Mitogen-Activated Protein Kinases / antagonists & inhibitors*
  • Models, Molecular
  • Phenols / chemical synthesis*
  • Phenols / pharmacology*
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology*
  • p38 Mitogen-Activated Protein Kinases


  • Enzyme Inhibitors
  • Phenols
  • Pyrimidines
  • Mitogen-Activated Protein Kinases
  • p38 Mitogen-Activated Protein Kinases