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Bioorg Med Chem Lett. 2011 Jul 1;21(13):4066-71. doi: 10.1016/j.bmcl.2011.04.121. Epub 2011 May 11.

Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.

Author information

1
Department of Medicinal Chemistry, Pfizer Corporation, 700 Chesterfield Parkway West, Chesterfield, MO 63017, United States. shaun.selness@gmail.com

Abstract

The synthesis and SAR studies of a novel N-aryl pyridinone class of p38 kinase inhibitors are described. Systematic structural modifications to the HTS lead, 5, led to the identification of (-)-4a as a clinical candidate for the treatment of inflammatory diseases. Additionally, the chiral synthesis and properties of (-)-4a are described.

PMID:
21641211
DOI:
10.1016/j.bmcl.2011.04.121
[Indexed for MEDLINE]

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