Novel carbohydrate-triazole derivatives as potential α-glucosidase inhibitors.
10.1016/S1875-5364(20)60013-9
- Author:
Zi-Pei ZHANG
1
;
Wan-Ying XUE
1
;
Jian-Xing HU
1
;
De-Cai XIONG
1
;
Yan-Fen WU
2
;
Xin-Shan YE
3
Author Information
1. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: wuyanfen@bjmu.edu.cn.
3. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: xinshan@bjmu.edu.cn.
- Publication Type:Journal Article
- Keywords:
Enzyme assay;
Molecular docking;
Pyrano[2, 3-d]trizaole;
α-Glucosidase inhibitor
- From:
Chinese Journal of Natural Medicines (English Ed.)
2020;18(10):729-737
- CountryChina
- Language:English
-
Abstract:
A series of novel pyrano[2, 3-d]trizaole compounds were synthesized and their α-glucosidase inhibitory activities were evaluated by in vitro enzyme assay. The experimental data demonstrated that compound 10f showed up to 10-fold higher inhibition (IC74.0 ± 1.3 μmol·L) than acarbose. The molecular docking revealed that compound 10f could bind to α-glucosidase via the hydrophobic, π-π stacking, and hydrogen bonding interactions. The results may benefit further structural modifications to find new and potent α-glucosidase inhibitors.