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ID: ALA1134856
Journal: Bioorg Med Chem Lett
Title: SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38MAP kinase inhibitors.
Authors: Revesz L, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Wolf R, Zimmerlin AG.
Abstract: 2,6-Diamino-3,5-difluoropyridinyl substituted pyridinylimidazoles, -pyrroles, -oxazoles, -thiazoles and -triazoles have been identified as novel p38alpha inhibitors. Pyridinylimidazole 11 potently inhibited LPS-induced TNFalpha in mice, showed good efficacy in the established rat adjuvant (ED(50): 10 mg/kg po b.i.d.) and collagen induced arthritis (ED(50): 5 mg/kg po b.i.d.) with disease modifying properties based on histological analysis of the joints.
CiteXplore: 12127515