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

J Dumas, H Hatoum-Mokdad, R Sibley, B Riedl…

Index: Dumas, Jacques; Hatoum-Mokdad, Holia; Sibley, Robert; Riedl, Bernd; Scott, William J.; Monahan, Mary Katherine; Lowinger, Timothy B.; Brennan, Catherine; Natero, Reina; Turner, Tiffany; Johnson, Jeffrey S.; Schoenleber, Robert; Bhargava, Ajay; Wilhelm, Scott M.; Housley, Timothy J.; Ranges, Gerald E.; Shrikhande, Alka Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 18 p. 2051 - 2054

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Citation Number: 91

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).