Quinolines as potent 5-lipoxygenase inhibitors: synthesis and biological profile of L-746,530.
作者： Daniel Dubé , Marc Blouin , Christine Brideau , Chi-Chung Chan , Sylvie Desmarais
DOI: 10.1016/S0960-894X(98)00201-7
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摘要: Abstract Leukotriene biosynthesis inhibitors have potential as new therapeutic agents for asthma and inflammatory diseases. A series of novel substituted 2-cyanoquinolines been synthesized the structure activity relationships were evaluated with respect to their ability inhibit formation leukotrienes via 5-lipoxygenase enzyme. [1 S ,5 R ]-2-Cyano-4-(3-furyl)-7-3-fluoro-5-[3-(3 α -hydroxy-6,8-dioxabicyclo[3.2.1]-octanyl)]phenoxymethyl quinoline (L-746,530) 3 represents a distinct class possesses in vitro vivo potency comparable or superior naphthalenic analog (L-739,010) 2 .
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