Novel 1H-benzimidazol-4-ols with potent 5-lipoxygenase inhibitory activity

DR Buckle, KA Foster, JF Taylor…

文献索引：Buckle, Derek R.; Foster, Keith A.; Taylor, John F.; Tedder, John M.; Thody, Veronica E.; et al. Journal of Medicinal Chemistry, 1987 , vol. 30, # 12 p. 2216 - 2221

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被引用次数: 23

摘要

The synthesis and structure-activity profile of 2-substituted benzimidazol-4-01s as inhibitors of cell-free RBL-1 5-lipoxygenase are discussed, and their potency is compared with that of the standard inhibitors phenidone, AA 861, BW 755C, and nordihydroguaiaretic acid. In contrast to the standard compounds, most did not inhibit the release of slow-reacting substance of anaphylaxis (SRS-A) in vivo when administered at 200 pM ip to rats ...