title: Synthesis and evaluation of the alpha-glucosidase inhibitory activity of 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives.
abstract: In the course of studies directed toward the discovery of novel non-sugar alpha-glucosidase inhibitors for the treatment of diabetes, a series of 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives was synthesized and evaluated as alpha-glucosidase inhibitors. Most compounds showed good inhibitory activity with IC(50) values ranging from 0.0645 microM to 26.746 microM. 7-Hydroxy-6-methoxy-3-[4-(4-methylphenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one 7u manifested the most potent inhibitory activity with an IC(50) value of 0.0645 microM.
authors.affiliation: Key Laboratory of New Drugs Design and Discovery of Liaoning Province, Shenyang Pharmaceutical University, 103 Culture Road, Shenhe District, Shenyang 110016, China. sjwang_99@yahoo.com.cn
authors.forename: Shaojie
authors.initials: S
authors.lastname: Wang
authors.forename: Jufang
authors.initials: J
authors.lastname: Yan
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Wang
authors.forename: Zhuo
authors.initials: Z
authors.lastname: Yang
authors.forename: Fengwei
authors.initials: F
authors.lastname: Lin
authors.forename: Tingjian
authors.initials: T
authors.lastname: Zhang
mesh_terms: D001578:Benzopyrans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D065089:Glycoside Hydrolase Inhibitors; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: C550202:7-hydroxy-6-methoxy-3-(4-(4-methylphenylsulfonamido)benzoyl)-2H-1-benzopyran-2-one; D001578:Benzopyrans; D003374:Coumarins; D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D013449:Sulfonamides