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Bioorg Med Chem Lett. 2009 Oct 15;19(20):5851-6. doi: 10.1016/j.bmcl.2009.08.082. Epub 2009 Aug 27.

Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase.

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1
Department of Medicinal Chemistry, Pfizer Corporation, 700 Chesterfield Parkway West, Chesterfield, MO 63017, USA. shaun.r.selness@pfizer.com

Abstract

The identification and evolution of a series of potent and selective p38 inhibitors is described. p38 inhibitors based on a N-benzyl pyridinone high-throughput screening hit were prepared and their SAR explored. Their design was guided by ligand bound co-crystals of p38alpha. These efforts resulted in the identification of 12r and 19 as orally active inhibitors of p38 with significant efficacy in both acute and chronic models of inflammation.

PMID:
19751974
DOI:
10.1016/j.bmcl.2009.08.082
[Indexed for MEDLINE]
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