Title of article
SAR of benzoylpyridines and benzophenones as p38α MAP kinase inhibitors with oral activity
Author/Authors
Laszlo Revesz، نويسنده , , Ernst Blum، نويسنده , , Franco E. Di Padova، نويسنده , , Thomas Buhl، نويسنده , , Roland Feifel، نويسنده , , Hermann Gram، نويسنده , , Peter Hiestand، نويسنده , , Ute Manning، نويسنده , , Gerard Rucklin، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
3601
To page
3605
Abstract
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: 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 po in CIA.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794645
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