1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors

  • Bioorg Med Chem Lett. 2000 Sep 18;10(18):2051-4. doi: 10.1016/s0960-894x(00)00272-9.
J Dumas  1 ,  H Hatoum-Mokdad ,  R Sibley ,  B Riedl ,  W J Scott ,  M K Monahan ,  T B Lowinger ,  C Brennan ,  R Natero ,  T Turner ,  J S Johnson ,  R Schoenleber ,  A Bhargava ,  S M Wilhelm ,  T J Housley ,  G E Ranges ,  A Shrikhande
Affiliations
  • 1. Department of Chemistry Research, Bayer Research Center, West Haven, CT 06516, USA. [email protected]
PMID: 10999468 DOI: 10.1016/s0960-894x(00)00272-9
Abstract

Inhibitors of the MAP kinase p38 are potentially useful for the treatment of arthritis and osteoporosis. Several 2,3-dichlorophenyl ureas were identified as small-molecule inhibitors of p38 by a combinatorial chemistry effort. Optimization for cellular potency led to the discovery of a new class of potent and selective p38 kinase inhibitors, exemplified by the 1-phenyl-5-pyrazolyl urea 7 (IC50 = 13 nM).