Small molecule antagonists of the CXCR2 and CXCR1 chemokine receptors as therapeutic agents for the treatment of inflammatory diseases

被引：59

作者：

Busch-Petersen, Jakob ^{[1
]}

机构：

[1] GlaxoSmithKline, King Of Prussia, PA 19406 USA

来源：

CURRENT TOPICS IN MEDICINAL CHEMISTRY | 2006年 / 6卷 / 13期

关键词：

CXCR2; CXCR1; IL-8; GRO alpha; neutrophil (PMN); chemotaxis; small molecule antagonist;

D O I：

10.2174/15680266106061345

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the past eight years, numerous series of small molecule CXCR2 and CXCR1 antagonists have been disclosed. These compounds have proved to be effective inhibitors of ELR+ chemokine-induced chemotaxis of neutrophils and other immune cells in vitro and have also been efficacious in several animal models of inflammatory disease. Although some of these compounds have been reported to be in clinical development, no data on clinical studies in patients with inflammatory disease has been revealed to date. This review details the medicinal chemistry and pharmacology of the aforementioned antagonist series.

引用

页码：1345 / 1352

页数：8

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