Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase.
Bioorganic & Medicinal Chemistry Letters(2011)
摘要
A series of inhibitors of mammalian 15-lipoxygenase (15-LO) based on a 3,4,5-tri-substituted pyrazole scaffold is described. Replacement of a sulfonamide functionality in the lead series with a sulfamide group resulted in improved physicochemical properties generating analogs with enhanced inhibition in cell-based and whole blood assays.
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关键词
15-Lipoxygenase,Inhibitors,Pyrazole,Sulfonamides,Sulfamides,Arachidonic acid,Linoleic acid
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