Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors

…, AM Boctor, DT Connor, CR Kostlan…

文献索引：Flynn; Belliotti; Boctor; Connor; Kostlan; Nies; Ortwine; Schrier; Sircar Journal of Medicinal Chemistry, 1991 , vol. 34, # 2 p. 518 - 525

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被引用次数: 95

摘要

A series of styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles were prepared and found to be dual inhibitors of 5-lipoxygenase and cyclooxygenase in rat basophilic leukemia cells. Compounds from this series also were found to inhibit the in vivo production of LTBl when dosed orally in rats. Among these compounds, di-tert-butylphenols 19 and 33 exhibit oral activity in various models of inflammation and, most importantly, are devoid of ulcerogenic ...