Diarylspiro [2.4] heptenes as orally active, highly selective cyclooxygenase-2 inhibitors: synthesis and structure-activity relationships

…, GD Anderson, AW Veenhuizen, Y Zhang…

文献索引：Huang, Horng-Chih; Li, James J.; Garland, Danny J.; Chamberlain, Timothy S.; Reinhard, Emily J.; Manning, Robert E.; Seibert, Karen; Koboldt, Carol M.; Gregory, Susan A.; Anderson, Gary D.; Veenhuizen, Amy W.; Zhang, Yan; Perkins, William E.; Burton, Earl G.; Cogburn, J. Nita; Isakson, Peter C.; Reitz, David B. Journal of Medicinal Chemistry, 1996 , vol. 39, # 1 p. 253 - 266

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被引用次数: 59

摘要

A novel series of 5, 6-diarylspiro [2.4] hept-5-enes was shown to provide highly potent and selective cyclooxygenase-2 (COX-2) inhibitors. A study of structure-activity relationships in this series suggests that 3, 4-disubstituted phenyl analogs are generally more selective than 4-substituted phenyl analogs and that replacement of the methyl sulfone group on the 6- phenyl ring with a sulfonamide moiety results in compounds with superior in vivo ...