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

作者信息

Dubé D, Blouin M, Brideau C, Chan C C, Desmarais S, Ethier D, Falgueyret J P, Friesen R W, Girard M, Girard Y, Guay J, Riendeau D, Tagari P, Young R N

机构信息

Merck Frosst Centre For Therapeutic Research, Québec, Canada.

出版信息

Bioorg Med Chem Lett. 1998 May 19;8(10):1255-60. doi: 10.1016/s0960-894x(98)00201-7.

DOI:10.1016/s0960-894x(98)00201-7
PMID:9871745
Abstract

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.

摘要

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