Author/Authors :
Jerry L. Adams، نويسنده , , Jeffrey C. Boehm، نويسنده , , Shouki Kassis، نويسنده , , Peter D. Gorycki، نويسنده , , Edward F. Webb، نويسنده , , Ralph Hall، نويسنده , , Margaret Sorenson، نويسنده , , John C. Lee، نويسنده , , Andrew Ayrton، نويسنده , , Don E. Griswold، نويسنده , , Timothy F. Gallagher، نويسنده ,
Abstract :
Pyrimidine analogs of the pyridinylimidazole class of CSBP/p38 kinase inhibitors were prepared in an effort to reduce the potent inhibition of hepatic cytochrome P450 observed for the pyridinyl compounds. The substitution of pyrimidin-4-yl, 2-methoxypyrimidin-4-yl, or 2-methylaminopyrimidin-4-yl for pyridin-4-yl effectively dissociates CSBP/p38 kinase from P450 inhibition for this series and furthermore achieves an increase in oral activity.
