Journal
CHINESE JOURNAL OF NATURAL MEDICINES
Volume 18, Issue 10, Pages 729-737Publisher
CHINESE JOURNAL NATURAL MEDICINES
DOI: 10.1016/S1875-5364(20)60013-9
Keywords
Pyrano[2, 3-d]trizaole; alpha-Glucosidase inhibitor; Enzyme assay; Molecular docking
Funding
- National Key R&D Program of China [2018YF-A0507602]
- National Natural Science Foundation of China [81821004, 21738001]
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A series of novel pyrano[2, 3-d]trizaole compounds were synthesized and their alpha-glucosidase inhibitory activities were evaluated by in vitro enzyme assay. The experimental data demonstrated that compound 10f showed up to 10-fold higher inhibition (IC50 74.0 +/- 1.3 mu mol.L-1) than acarbose. The molecular docking revealed that compound 10f could bind to alpha-glucosidase via the hydrophobic, pi-pi stacking, and hydrogen bonding interactions. The results may benefit further structural modifications to find new and potent a-glucosidase inhibitors.
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