title: Sulfonamide chalcone as a new class of alpha-glucosidase inhibitors.
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.
authors.affiliation: 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.
authors.forename: Woo Duck
authors.initials: WD
authors.lastname: Seo
authors.forename: Jin Hyo
authors.initials: JH
authors.lastname: Kim
authors.forename: Jae Eun
authors.initials: JE
authors.lastname: Kang
authors.forename: Hyung Won
authors.initials: HW
authors.lastname: Ryu
authors.forename: Marcus J
authors.initials: MJ
authors.lastname: Curtis-Long
authors.forename: Hyun Sun
authors.initials: HS
authors.lastname: Lee
authors.forename: Min Suk
authors.initials: MS
authors.lastname: Yang
authors.forename: Ki Hun
authors.initials: KH
authors.lastname: Park
mesh_terms: D047188:Chalcones / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D065089:Glycoside Hydrolase Inhibitors; D007700:Kinetics; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D000516:alpha-Amylases / Q000378:metabolism; D001614:beta-Amylase / Q000378:metabolism
chemical_list: D047188:Chalcones; D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D013449:Sulfonamides; D000516:alpha-Amylases; D001614:beta-Amylase