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Synthesis and pharmacological characterization of a potent,orally active p38 kinase inhibitor |
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| Authors: | Dumas Jacques Hatoum-Mokdad Holia Sibley Robert N Smith Roger A Scott William J Khire Uday Lee Wendy Wood Jill Wolanin Donald Cooley Jeffrey Bankston Donald Redman Aniko M Schoenleber Robert Caringal Yolanda Gunn David Romero Romulo Osterhout Martin Paulsen Holger Housley Timothy J Wilhelm Scott M Pirro John Chien Du-Shieng Ranges Gerald E Shrikhande Alka Muzsi Andrew Bortolon Elizabeth Wakefield Jean Gianpaolo Ostravage Cynthia Bhargava Ajay Chau Thuy |
| Institution: | Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA. jacques.dumas.b@bayer.com |
| Abstract: | Inhibitors of the MAP kinase p38 provide a novel approach for the treatment of osteoporosis, inflammatory disorders, and cancer. We have identified N-(3-tert-butyl-1-methyl-5-pyrazolyl)-N'-(4-(4-pyridinylmethyl)phenyl)urea as a potent and selective p38 kinase inhibitor in biochemical and cellular assays. This compound is orally active in two acute models of cytokine release (TNF-induced IL-6 and LPS-induced TNF) and a chronic model of arthritis (20-day murine collagen-induced arthritis). |
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