Literature

Abstract

A novel series of 1,6-bis-triazole-benzyl-α-glucoside derivatives (7a-7ee) were designed, synthesized and evaluated for inhibitory activity against α-glucosidase. Most of the synthesized compounds exhibited good activity with IC<sub>50</sub> ranging from 3.73 µM to 53.34 µM and are more potent than the standard drug acarbose (IC<sub>50</sub> = 146.25 ± 0.40 µM). SARs study showed the ester and menthol moiety play an important role in the inhibitory activity. The molecular docking model of the potent compounds 7f, 7z, 7cc and 7dd showed good binding energy and interacts well with amino acid residues around the active site of the enzyme, which confirmed the in vitro activity results.

DOI： 10.1016/j.bmcl.2021.128331

Synthesis and biological evaluation of 1,6-bis-triazole-2,3,4-tri-O-benzyl-α-d-glucopyranosides as a novel α-glucosidase inhibitor in the treatment of Type 2 diabetes

Bioorganic & Medicinal Chemistry Letters 2021.0

Synthesis, in vitro evaluation and molecular docking studies of novel triazine-triazole derivatives as potential α-glucosidase inhibitors

European Journal of Medicinal Chemistry 2017.0

Synthesis and biological evaluation of novel 1,2,4-triazine derivatives bearing carbazole moiety as potent α-glucosidase inhibitors

Bioorganic & Medicinal Chemistry Letters 2016.0

Synthesis, Biological Activity, and Molecular Modeling Studies of 1H-1,2,3-Triazole Derivatives of Carbohydrates as α-Glucosidases Inhibitors

Journal of Medicinal Chemistry 2010.0

Design, synthesis, in vitro, and in silico studies of novel diarylimidazole-1,2,3-triazole hybrids as potent α-glucosidase inhibitors

Bioorganic & Medicinal Chemistry 2019.0

Quinazolinone-1,2,3-triazole-acetamide conjugates as potent α-glucosidase inhibitors: synthesis, enzyme inhibition, kinetic analysis, and molecular docking study