A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis

被引：25

作者：

Brown, DS ^{[1
]}

Belfield, AJ ^{[1
]}

Brown, GR ^{[1
]}

Campbell, D ^{[1
]}

Foubister, A ^{[1
]}

Masters, DJ ^{[1
]}

Pike, KG ^{[1
]}

Snelson, WL ^{[1
]}

Wells, SL ^{[1
]}

机构：

[1] AstraZeneca, Macclesfield SK10 4TG, Cheshire, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 21期

关键词：

p38 MAP kinase inhibitors;

D O I：

10.1016/j.bmcl.2004.08.006

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel p38 MAP kinase inhibitor structural class was discovered through selectivity screening. The rational analogue design, synthesis and structure-activity relationship of this series of bisamide inhibitors is reported. The inhibition in vitro of human p38alpha enzyme activity and lipopolysaccharide-induced tumour necrosis factor-alpha release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5383 / 5387

页数：5

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