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Synthesis ofN-phenylphthalimide Derivatives as α-Glucosidase Inhibitors

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  • Drug discovery
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Abstract

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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Correspondence to Wanchai Pluempanupat.

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Pluempanupat, W., Adisakwattana, S., Yibchok-Anun, S. et al. Synthesis ofN-phenylphthalimide Derivatives as α-Glucosidase Inhibitors. Arch Pharm Res 30, 1501–1506 (2007). https://doi.org/10.1007/BF02977317

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