2. Academic Validation
  3. 1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors

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

Affiliation

  • 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).

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