Author/Authors :
Laszlo Revesz، نويسنده , , Ernst Blum، نويسنده , , Franco E. Di Padova، نويسنده , , Thomas Buhl، نويسنده , , Roland Feifel، نويسنده , , Hermann Gram، نويسنده , , Peter Hiestand، نويسنده , , Ute Manning، نويسنده , , Gerard Rucklin، نويسنده ,
Abstract :
Benzoylpyridines and benzophenones were synthesized and evaluated in vitro as p38α inhibitors and in vivo in several models of rheumatoid arthritis. Oral activity was found to depend upon substitution: 1,1-dimethylpropynylamine substituted benzophenone 10b (IC50: 14 nM) and pyridinoyl substituted benzimidazole 17b (IC50: 21 nM) showed highest efficacy and selectivity with ED50s of 9.5 and 8.6 mg/kg po in CIA.
