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Antiinflammatory 2, 6-di-tert-butyl-4-(2-arylethenyl) phenols

…, HC Wong, GJ Possanza, AG Graham…

文献索引:Lazer, Edward S.; Wong, Hin-Chor; Possanza, Genus J.; Graham, Anne G.; Farina, Peter R. Journal of Medicinal Chemistry, 1989 , vol. 32, # 1 p. 100 - 104

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被引用次数: 46

摘要

A series of 2, 6-di-tert-butyl-4-(2-arylethenyl) phenols was prepared and examined for their ability to inhibit cyclooxygenase and 5-lipoxygenase in vitro and developing adjuvant arthritis in vivo in the rat. Structure-activity relationships are discussed. Among the best compounds is (E)-2, 6-di-tert-buty1-4-[2-(3-pyridinyl) ethenyl] phenol (7d). It has an IC,, of 0.67 pM for cyclooxygenase and 2.7 pM for 5-lipoxygenase and an ED,, of 2.1 mg/kg in ...