Sulfonamide chalcone as a new class of alpha-glucosidase inhibitors |
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Authors: | Seo Woo Duck Kim Jin Hyo Kang Jae Eun Ryu Hyung Won Curtis-Long Marcus J Lee Hyun Sun Yang Min Suk Park Ki Hun |
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Institution: | Division of Applied Life Science (BK21 Program), Department of Agricultural Chemistry, Institute of Agriculture & Life Sciences, Gyeongsang National University, Jinju 660-701, Republic of Korea. |
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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 (alpha-glucosidase, alpha-amylase, and beta-amylase) inhibitory activities. In particular, sulfonamide chalcones 17-20 had more potent alpha-glucosidase inhibitory activity than aminated chalcone 13-16. 4'-(p-Toluenesulfonamide)-3,4-dihydroxy chalcone 20 (IC(50)=0.4microM) was the best inhibitor against alpha-glucosidase, and these sulfonamide chalcones showed non-competitive inhibition. |
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Keywords: | Chalcone Sulfonamide chalcone α -Glucosidase inhibitor Amylase |
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