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 , , Alfred G. Zimmerlin، نويسنده ,
Abstract :
The 4-hydroxypiperidine substituent was found to confer high p38 selectivity devoid of COX-1 affinity, when attached to a series of pyridinyl substituted heterocycles. Pyridinyloxazole 11 showed a promising in vivo profile with bioavailability of 64% and ED50 in rat collagen induced arthritis of 10 mg/kg po bid. In contrast to pyridinylimidazoles such as SB 203580, 11 did not inhibit human cytochrome P450 isoenzymes.
