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

Revesz, Laszlo and Blum, Ernst and Di Padova, Franco E. and Buhl, Thomas and Feifel, Roland and Gram, Hermann and Hiestand, Peter and Manning, Ute and Rucklin, Gerard (2004) SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity. Bioorganic & Medicinal Chemistry Letters, 14 (13). pp. 3601-3605. ISSN 0960-894X

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.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
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Date Deposited: 14 Dec 2009 13:55
Last Modified: 31 Jan 2013 01:07
URI: https://oak.novartis.com/id/eprint/750

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