Document Report Card
Basic Information
ID: ALA1147484
Journal: Bioorg Med Chem Lett
Title: SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.
Authors: Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Rucklin G.
Abstract: Benzoylpyridines and benzophenones were synthesized and evaluated in vitro as p38alpha 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 p.o. in CIA.
CiteXplore: 15177483