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The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors |
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| Authors: | Montalban Antonio Garrido Boman Erik Chang Chau-Dung Ceide Susana Conde Dahl Russell Dalesandro David Delaet Nancy G J Erb Eric Ernst Justin T Gibbs Andrew Kahl Jeffrey Kessler Linda Lundström Jan Miller Stephen Nakanishi Hiroshi Roberts Edward Saiah Eddine Sullivan Robert Wang Zhijun Larson Christopher J |
| Institution: | Drug Discovery, Kémia, Inc., 5871 Oberlin Drive, Suite 100, San Diego, CA 92121, USA. catalaba@hotmail.com |
| Abstract: | We have identified a novel series of potent p38 MAP kinase inhibitors through structure-based design which due to their extended molecular architecture bind, in addition to the ATP site, to an allosteric pocket. In vitro ADME and in vivo PK studies show these compounds to have drug-like characteristics which could result in the development of an oral treatment for inflammatory conditions. |
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