Synthesis and Molecular Docking Studies of Alkoxy- and Imidazole-Substituted Xanthones as α-Amylase and α-Glucosidase Inhibitors.

ABSTRACT: Current antidiabetic drugs have severe side effects, which may be minimized by new selective molecules that strongly inhibit α-glucosidase and weakly inhibit α-amylase. We have synthesized novel alkoxy-substituted xanthones and imidazole-substituted xanthones and have evaluated them for their in silico and in vitro α-glucosidase and α-amylase inhibition activity. Compounds 6c, 6e, and 9b promoted higher α-glucosidase inhibition (IC₅₀ = 16.0, 12.8, and 4.0 µM, respectively) and lower α-amylase inhibition (IC₅₀ = 76.7, 68.1, and >200 µM, respectively) compared to acarbose (IC₅₀ = 306.7 µM for α-glucosidase and 20.0 µM for α-amylase). Contrarily, derivatives 10c and 10f showed higher α-amylase inhibition (IC₅₀ = 5.4 and 8

SUBMITTER: Aguila-Munoz DG 

PROVIDER: S-EPMC10222686 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature