Title of article :
SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38 MAP kinase inhibitors
Author/Authors :
Laszlo Revesz، نويسنده , , Franco E. Di Padova، نويسنده , , Thomas Buhl، نويسنده , , Roland Feifel، نويسنده , , Hermann Gram، نويسنده , , Peter Hiestand، نويسنده , , Ute Manning، نويسنده , , Romain Wolf، نويسنده , , Alfred G. Zimmerlin، نويسنده ,
Abstract :
2,6-Diamino-3,5-difluoropyridinyl substituted pyridinylimidazoles, -pyrroles, -oxazoles, -thiazoles and -triazoles have been identified as novel p38α inhibitors. Pyridinylimidazole 11 potently inhibited LPS-induced TNFα in mice, showed good efficacy in the established rat adjuvant (ED50: 10 mg/kg po b.i.d.) and collagen induced arthritis (ED50: 5 mg/kg po b.i.d.) with disease modifying properties based on histological analysis of the joints.
