Abstract
To discover potent α-glucosidase inhibitors, a class of novel triazole-phenylacetamide derivatives (5a-5p) were designed, prepared, and tested for their α-glucosidase inhibitory effects. All tested compounds (5a-5p) displayed a strong α-glucosidase inhibitory activity (IC50 = 6.69 ± 0.18–113.65 ± 2.94 μM) in comparison with the positive control acarbose (IC50 = 723.06 ± 11.26 μM). Thereinto, 5g (IC50 = 6.69 ± 0.18 μM) showed the best anti-α-glucosidase activity and behaved as a mixed-type inhibitor with the value of Ki and Kis to be 1.65 μM and 4.54 μM, respectively. Besides, fluorescence quenching experiment, three-dimensional fluorescence spectra assay, circular dichroism analysis, and molecular docking studies indicated that 5g may inhibit α-glucosidase activity by binding with its active site as well as changing the secondary structure of α-glucosidase. Combined with the inhibition effect on the rise of postprandial blood glucose level and low cytotoxicity of 5g, it could be concluded that these title compounds may play a role as lead compounds to develop novel α-glucosidase inhibitors.
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