In:
Frontiers in Chemistry, Frontiers Media SA, Vol. 10 ( 2022-6-23)
Abstract:
α-Glucosidase inhibitors are known to prevent the digestion of carbohydrates and reduce the impact of carbohydrates on blood glucose. To develop novel α-glucosidase inhibitors, a series of 5-fluoro-2-oxindole derivatives ( 3a ∼ 3v ) were synthesized, and their α-glucosidase inhibitory activities were investigated. Biological assessment results showed that most synthesized compounds presented potential inhibition on α-glucosidase. Among them, compounds 3d , 3f , and 3i exhibited much better inhibitory activity with IC 50 values of 49.89 ± 1.16 μM, 35.83 ± 0.98 μM, and 56.87 ± 0.42 μM, respectively, which were about 10 ∼ 15 folds higher than acarbose (IC 50 = 569.43 ± 43.72 μM). A kinetic mechanism study revealed that compounds 3d , 3f , and 3i inhibited the α-glucosidase in a reversible and mixed manner. Molecular docking was carried out to simulate the affinity between the compound and α-glucosidase.
Type of Medium:
Online Resource
ISSN:
2296-2646
DOI:
10.3389/fchem.2022.928295
DOI:
10.3389/fchem.2022.928295.s001
Language:
Unknown
Publisher:
Frontiers Media SA
Publication Date:
2022
detail.hit.zdb_id:
2711776-5