| Literature DB >> 15177483 |
Laszlo Revesz1, Ernst Blum, Franco E Di Padova, Thomas Buhl, Roland Feifel, Hermann Gram, Peter Hiestand, Ute Manning, Gerard Rucklin.
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.Entities:
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Year: 2004 PMID： 15177483 DOI： 10.1016/j.bmcl.2004.03.111
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823