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联苯酰胺p38激酶抑制剂3:细胞活性和体内活性的改善

Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.

作者信息

Angell Richard, Aston Nicola M, Bamborough Paul, Buckton Jacky B, Cockerill Stuart, deBoeck Suzanne J, Edwards Chris D, Holmes Duncan S, Jones Katherine L, Laine Dramane I, Patel Shila, Smee Penny A, Smith Kathryn J, Somers Don O, Walker Ann L

机构信息

GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.

出版信息

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4428-32. doi: 10.1016/j.bmcl.2008.06.048. Epub 2008 Jun 18.

Abstract

The biphenyl amides (BPAs) are a novel series of p38alpha MAP kinase inhibitor. The optimisation of the series to give compounds that are potent in an in vivo disease model is discussed. SAR is presented and rationalised with reference to the crystallographic binding mode.

摘要

联苯酰胺(BPAs)是一类新型的p38α丝裂原活化蛋白激酶抑制剂。本文讨论了该系列化合物的优化,以获得在体内疾病模型中有效的化合物。文中介绍了构效关系,并根据晶体学结合模式进行了合理分析。

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