Quinolines as potent 5-lipoxygenase inhibitors:: Synthesis and biological profile of L-746,530

被引：316

作者：

Dubé, D ^{[1
]}

Blouin, M ^{[1
]}

Brideau, C ^{[1
]}

Chan, CC ^{[1
]}

Desmarais, S ^{[1
]}

Ethier, D ^{[1
]}

Falgueyret, JP ^{[1
]}

Friesen, RW ^{[1
]}

Girard, M ^{[1
]}

Girard, Y ^{[1
]}

Guay, J ^{[1
]}

Riendeau, D ^{[1
]}

Tagari, P ^{[1
]}

Young, RN ^{[1
]}

机构：

[1] Merck Frosst Ctr Therapeut Res, Dorval, PQ H9R 4P8, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(98)00201-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Leukotriene biosynthesis inhibitors have potential as new therapeutic agents for asthma and inflammatory diseases. A series of novel substituted 2-cyanoquinolines have been synthesized and the structure activity relationships were evaluated with respect to their ability to inhibit the formation of leukotrienes via the 5-lipoxygenase enzyme. [1S,5R]-2-Cyano-4-(3-furyl)-7-{3-fluoro-5-[3-(3 alpha-hydroxy-6,8-dioxabicyclo[3.2.1]octanyl)]phenoxymethyl}quinoline (L-746,530) 3 represents a distinct class of inhibitors and possesses in vitro and in vivo potency comparable or superior to naphthalenic analog (L-739,010) 2. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1255 / 1260

页数：6

共 21 条

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