Sulfonamide chalcone as a new class of α-glucosidase inhibitors

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Title
Sulfonamide chalcone as a new class of α-glucosidase inhibitors
Author(s)
W D Seo; J H Kim; J E Kang; Hyung Won Ryu; M J Curtis-Long; Hyun Sun Lee; M S Yang; K H Park
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 15, no. 24, pp. 5514-5516
Publication Year
2005
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 (IC50 = 0.4 μM) was the best inhibitor against α-glucosidase, and these sulfonamide chalcones showed non-competitive inhibition.
Keyword
α-glucosidase inhibitoramylasechalconesulfonamide chalcone
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2005.08.087
Type
Article
Appears in Collections:
Ochang Branch Institute > Natural Product Research Center > 1. Journal Articles
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