期刊
MEDICINAL CHEMISTRY RESEARCH
卷 29, 期 5, 页码 868-876出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-020-02522-7
关键词
Phthalimide; Benzamide; 1,2,3-Triazole; Hybrid; alpha-Glucosidase
A new series of phthalimide-benzamide-1,2,3-triazole hybrids 8a-k as alpha-glucosidase inhibitors was designed and synthesized. The biological evaluation of compounds 8a-k against yeast alpha-glucosidase demonstrated that all they have excellent inhibitory activity in comparison with standard inhibitor acarbose. Among them, the most potent compound was compound 8d with inhibitory activity 18.5-fold more than acarbose. Kinetic study revealed that alpha-glucosidase inhibition of compound 8d was the competitive type. Furthermore, docking study suggested that compound 8d is more stable than acarbose in the active site of alpha-glucosidase.
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