Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl) amino] oxoalkanoic acid esters

…, DM Kubrak, J Chang, SM DiZio, M Hite…

文献索引：Musser; Kubrak; Chang; DiZio; Hite; Hand; Lewis Journal of medicinal chemistry, 1987 , vol. 30, # 2 p. 400 - 405

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被引用次数: 30

摘要

A series of novel benzoheterocyclic [(methoxyphenyl) amino] oxoalkanoic acid esters has been prepared. These compounds were tested as inhibitors of rat polymorphonuclear leukocyte 5-lipoxgenase (LO) in vitro and as inhibitors of leukotriene D,(LTD4) and ovalbumin (OA) induced bronchospasm in the guinea pig (GP) in vivo. In general, inhibitory activity against 5-L0, LTD4, and OA was broadest for benzthiazole-containing analogues ( ...