SAR of benzoylpyridines and benzophenones as p38α MAP kinase inhibitors with oral activity

…, E Blum, FE Di Padova, T Buhl, R Feifel, H Gram…

文献索引：Revesz, Laszlo; Blum, Ernst; Di Padova, Franco E.; Buhl, Thomas; Feifel, Roland; Gram, Hermann; Hiestand, Peter; Manning, Ute; Rucklin, Gerard Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 13 p. 3601 - 3605

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被引用次数: 55

摘要

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 8.6 mg/kg po in CIA.