SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.

@article{Rvsz2004SAROB,
  title={SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.},
  author={L. R{\'e}v{\'e}sz and E. Blum and F. D. di Padova and T. Buhl and R. Feifel and H. Gram and P. Hiestand and U. Manning and Gerard Rucklin},
  journal={Bioorganic & medicinal chemistry letters},
  year={2004},
  volume={14 13},
  pages={
          3601-5
        }
}
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. 
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