Author/Authors :
Swaminathan R. Natarajan، نويسنده , , Luping Liu، نويسنده , , Mark Levorse، نويسنده , , James E. Thompson، نويسنده , , Edward A. O’Neill، نويسنده , , Stephen J. O’Keefe، نويسنده , , Kalpit A. Vora، نويسنده , , Raymond Cvetovich، نويسنده , , John Y. Chung، نويسنده , , Ester Carballo-Jane، نويسنده , , Denise M. Visco، نويسنده ,
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 EC50 doses as low as 0.2 mpk.
Keywords :
7-Amino-naphthyridones , p38 MAP kinase inhibitors , Peptide flip , Rat LPS challenge
