Journal of medicinal chemistry

Chiral dioxolane inhibitors of leukotriene biosynthesis: Structure-activity relationships and syntheses using asymmetric dihydroxylation

GC Crawley, MT Briggs

文献索引：Crawley, Graham C.; Briggs, Malcolm T. Journal of Medicinal Chemistry, 1995 , vol. 38, # 20 p. 3951 - 3956

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被引用次数: 17

摘要

1, 3-Dioxolanes have been described as chiral inhibitors of 5-lipoxygenase (5LO). In the present work, this series has been developed further to provide agents which showed comparable or superior potency in vivo to ZD2138, a methoxytetrahydropyran inhibitor of 5L0, which is currently undergoing clinical evaluation. An asymmetric synthesis was developed to these dioxolanes based on asymmetric dihydroxylation.(S)-N-Methyl-4'-[[4-( ...