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ID: ALA1137291
Journal: Bioorg Med Chem Lett
Title: p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold.
Authors: Natarajan SR, Liu L, Levorse M, Thompson JE, O'Neill EA, O'Keefe SJ, Vora KA, Cvetovich R, Chung JY, Carballo-Jane E, Visco DM.
Abstract: A new sub-class of p38 inhibitors represented by 7-amino-naphthyridone have been discovered. Benchmark compound 16 potently inhibited p38 in vitro, was functionally active, and displayed excellent pharmacokinetic profiles in two animal species. Compound 16 reduced inflammation in animal disease models at EC(50) doses as low as 0.2mpk.
CiteXplore: 16945534