724767-82-2Relevant academic research and scientific papers
SAR of benzoylpyridines and benzophenones as p38α MAP kinase inhibitors with oral activity
Revesz, Laszlo,Blum, Ernst,Di Padova, Franco E.,Buhl, Thomas,Feifel, Roland,Gram, Hermann,Hiestand, Peter,Manning, Ute,Rucklin, Gerard
, p. 3601 - 3605 (2007/10/03)
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: 14nM) and pyridinoyl substituted benzimidazole 17b (IC50: 21nM) showed highest efficacy and selectivity with ED50s of 9.5 and 8.6mg/kg po in CIA.
