Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR

被引：28

作者：

Angell, Richard M. ^{[1
]}

Angell, Tony D. ^{[1
]}

Bamborough, Paul ^{[1
]}

Brown, David ^{[1
]}

Brown, Murray ^{[1
]}

Buckton, Jacky B. ^{[1
]}

Cockerill, Stuart G. ^{[1
]}

Edwards, Chris D. ^{[1
]}

Jones, Katherine L. ^{[1
]}

Longstaff, Tim ^{[1
]}

Smee, Penny A. ^{[1
]}

Smith, Kathryn J. ^{[1
]}

Somers, Don O. ^{[1
]}

Walker, Ann L. ^{[1
]}

Willson, Malcolm ^{[1
]}

机构：

[1] GlaxoSmithKline R&D, Med Res Ctr, Stevenage SG1 2NY, Herts, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 01期

关键词：

Binding mode; biphenyl amide; biphenyl amides; BPA; BPAs; CSBP; Inhibitors; Kinase selectivity; MAP kinase; p38; kinase; p38α; Protein kinase X-ray structure; Structure-based drug design;

D O I：

10.1016/j.bmcl.2007.10.043

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The biphenyl amides are a novel series of p38 MAP kinase inhibitors. Structure-activity relationships of the series against p38 alpha are discussed with reference to the X-ray crystal structure of an example. The series was optimised rapidly to a compound showing oral activity in an in vivo disease model. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：324 / 328

页数：5