AUTHOR=Zhu Hua , Zhong Xin 

TITLE=Synthesis of activity evaluation of flavonoid derivatives as ɑ-glucosidase inhibitors

JOURNAL=Frontiers in Chemistry

VOLUME=Volume 10 - 2022

YEAR=2022

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2022.1041328

DOI=10.3389/fchem.2022.1041328

ISSN=2296-2646

ABSTRACT=Six flavonoid derivatives were synthesized and tested for anti-α-glucosidase activities. All derivatives were confirmed using NMR and HRMS and exhibited excellent inhibitory effects on α-glucosidase. Derivative 4 exhibited the highest anti-α-glucosidase activity (IC50: 15.71 ± 0.21 μM). Inhibitory mechnism and inhibition kinetics results showed derivative 4 was a reversible and mixed-type inhibitor. Molecular docking revealed that derivative 4 was tightly bind to the amino acid residues of active pocket of α-glucosidase. This results also showed that the hybridization of flavonoid and phenylpropionic acid would be a useful strategy for the development of α-glucosidase inhibitors.