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  • Title: Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment.
    Author: Weinstein DS, Liu W, Ngu K, Langevine C, Combs DW, Zhuang S, Chen C, Madsen CS, Harper TW, Robl JA.
    Journal: Bioorg Med Chem Lett; 2007 Sep 15; 17(18):5115-20. PubMed ID: 17656086.
    Abstract:
    A series of 2,4,5-tri-substituted imidazoles has proven to be highly potent in inhibiting mammalian 15-lipoxygenase (15-LO) with excellent selectivity over human isozymes 5- and P-12-LO. Non-symmetrical sulfamides (e.g., 21a-n) were found to be suitable replacements for the earlier arylsulfonamide-containing members of this series (e.g., 2, 14a-p). Several members of these series also demonstrated potent inhibition of human 15-LO in a cell-based assay.
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