The design and synthesis of novel α-ketoamide-based p38 MAP kinase inhibitors

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• 作者：Antonio Garrido Montalban ; Erik Boman ; Chau-Dung Chang ; Susana Conde Ceide ; Russell Dahl ; David Dales ; ro ; Nancy G.J. Delaet ; Eric Erb ; Justin T. Ernst ; Andrew Gibbs ; Jeffrey Kahl ; Linda Kessler ; Jan L
• 关键词：p38 MAP kinase ; Antiinflammatory ; SAR ; Ketoamides ; Cytokines ; Drug-like
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 March 2008
• 卷：18
• 期：6
• 页码：1772-1777
• 文件大小：197 K

摘要

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.