Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment |
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Authors: | Weinstein David S Liu Wen Ngu Khehyong Langevine Charles Combs Donald W Zhuang Shaobin Chen Cindy Madsen Cort S Harper Timothy W Robl Jeffrey A |
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Affiliation: | Department of Discovery Chemistry, Bristol-Myers Squibb, Research and Development, PO Box 4000, Princeton, NJ 08543-5400, USA. david.weinstein@bms.com |
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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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