Dioxabicyclooctanyl naphthalenenitriles as nonredox 5-lipoxygenase inhibitors: structure-activity relationship study directed toward the improvement of metabolic …

…, JP Falgueyret, R Fortin, J Guay, P Hamel…

文献索引：Delorme, Daniel; Ducharme, Yves; Brideau, Christine; Chan, Chi-Chung; Chauret, Nathalie; Desmarais, Sylvie; Dube, Daniel; Falgueyret, Jean-Pierre; Fortin, Rejean; Guay, Jocelyne; Hamel, Pierre; Jones, Tom R.; Lepine, Carole; Li, Chun; McAuliffe, Malia; McFarlane, Cyril S.; Nicoll-Griffith, Deborah A.; Riendeau, Denis; Yergey, James A.; Girard, Yves Journal of Medicinal Chemistry, 1996 , vol. 39, # 20 p. 3951 - 3970

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被引用次数: 48

摘要

Naphthalenic lignan lactone 3a (L-702,539), a potent and selective 5-lipoxygenase (5-LO) inhibitor, is extensively metabolized at two different sites: the tetrahydropyran and the lactone rings. Early knowledge of the metabolic pathways triggered and directed a structure- activity relationship study aimed toward the improvement of metabolic stability in this series. The best modifications discovered, ie., replacement of the lactone ring by a nitrile group, ...