Synthesis and Evaluation of Phenyltriazole-Deoxynojirimycin Hybrids as Potent α-Glucosidase Inhibitors.

ABSTRACT: 1-deoxynojirimycin (DNJ) is a well-known α-glucosidase inhibitor. A series of phenyltriazole-deoxynojirimycin hybrids containing C₄ and C₆ (4 and 6 methylenes, respectively) linkers were synthesized. These novel compounds were assessed for preliminary glucosidase inhibition and cytotoxicity tests in vitro. Among them, compounds 12-14 and 16-20 (IC₅₀: 105 ± 9-11 ± 1 μM) were more active than deoxynojirimycin (DNJ, IC₅₀ = 155 ± 15 μM). The kinetics of enzyme inhibition measured by using Lineweaver-Burk plots indicated that compounds 18 and 19 were competitive inhibitors. In addition, a molecular docking study of α-glucosidase revealed that the interaction modes and the orientations of compound 18 and

SUBMITTER: Wang L 

PROVIDER: S-EPMC11547804 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature