Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase
Journal Article
·
· Bioorg. Med. Chem. Lett.
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 p38{alpha}. 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.
- Research Organization:
- Argonne National Lab. (ANL), Argonne, IL (United States)
- Sponsoring Organization:
- USDOE
- OSTI ID:
- 1006145
- Journal Information:
- Bioorg. Med. Chem. Lett., Vol. 19, Issue (20) ; 10, 2009; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- ENGLISH
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