In order to find new α-glucosidase inhibitors with high efficiency and low toxicity, novel chromone-based benzohydrazide derivatives 6a-6s were synthesized and characterized through 1H NMR, 13C NMR, and HRMS. All the new synthesized compounds were tested for inhibitory activities against α-glucosidase. Compounds 6a-6s with IC50 values ranging from 4.51 ± 0.09 to 27.21 ± 0.83 μM, showed a potential α-glucosidase inhibitory activity as compared to the positive control (acarbose: IC50 = 790.40 ± 0.91 μM). Compound 6i exhibited the highest α-glucosidase inhibitory activity with an IC50 value of 4.51 ± 0.09 μM. Theinteractionbetween α-glucosidase and 6i was further confirmed by enzyme kinetic, fluorescence quenching, circular dichroism, and molecular docking study. In vivo experiment showed that 6i could suppress the rise of blood glucose levels after sucrose loading. The cytotoxicity result indicated that 6i exhibited low cytotoxicity in vitro.
Keywords: Chromone; Circular dichroism spectra; Fluorescence quenching; α-Glucosidase inhibitor.
Copyright © 2022 Elsevier Inc. All rights reserved.