Abstract
Chalcones 1– 20, a new class of glycosidase inhibitors, were synthesized, and their glycosidase inhibitory activities were investigated. Non-aminochalcones 1– 12 had no inhibitory activity, however, aminochalcones 13– 20 had strong glycosidase (α-glucosidase, α-amylase, and β-amylase) inhibitory activities. In particular, sulfonamide chalcones 17– 20 had more potent α-glucosidase inhibitory activity than aminated chalcone 13– 16. 4′-( p-Toluenesulfonamide)-3,4-dihydroxy chalcone 20 (IC 50 = 0.4 μM) was the best inhibitor against α-glucosidase, and these sulfonamide chalcones showed non-competitive inhibition.
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