Synthesis ofN-phenylphthalimide Derivatives as α-Glucosidase Inhibitors

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作者
Wanchai Pluempanupat
Sirichai Adisakwattana
Sirintorn Yibchok-Anun
Warinthorn Chavasiri
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[1] Chulalongkorn University,Natural Products Research Unit, Department of Chemistry, Faculty of Science
[2] Chulalongkorn University,Department of Pharmacology, Faculty of Veterinary Science
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-Phenylphthalimide; α-Glucosidase; Diabetes;
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摘要
SixteenN-phenylphthalimide derivatives were synthesized and their ability to inhibit α-glucosidase was investigated.N-(2,4-dinitrophenyl)phthalimide was a potent inhibitor of yeast α-glucosidase (IC50; 0.158 ± 0.005 mM) and maltase (IC50; 0.051 ± 0.008 mM), whereas it did not inhibit sucrase. From a Lineweaver-Burk plot of α-glucosidase kinetics,N-(2,4-dichlorophenyl) phthalimide was found to be a competitive inhibitor of yeast α-glucosidase. These results indicate thatN-(2,4-dinitrophenyl)phthalimide could be a representative of a new group of α-glucosidase inhibitors.
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