Author/Authors :
Daniel Dubé، نويسنده , , Marc Blouin، نويسنده , , Christine Brideau، نويسنده , , Chi-Chung Chan، نويسنده , , Sylvie Desmarais، نويسنده , , Diane Ethier، نويسنده , , Jean-Pierre Falgueyret، نويسنده , , Richard W. Friesen، نويسنده , , Mario Girard، نويسنده , , Jean-Yves Girard، نويسنده , , Jocelyne Guay، نويسنده , , Denis Riendeau، نويسنده , , Philip Tagari، نويسنده , , Robert N. ، نويسنده ,
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-(3α-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.
