Tehran University of Medical Sciences

Science Communicator Platform

Share By
Novel 4-Formyl-1,3-Phenylene-Bisoxy-Bis(Methylene)-Bis(1,2,3-Triazole-N-Phenylacetamide) Derivatives As a New Category of Excellent Α-Glucosidase Inhibitors Publisher



Bakhshi Varzaneh S ; Sayahi M H ; Halimi M ; Ghafouri S N ; Dastyafteh N ; Mojtabavi S ; Larijani B ; Mohammadi Khanaposhtani M ; Mahdavi M
Authors

Source: RSC Advances Published:2026


Abstract

A series of thirteen new 4-formyl-1,3-phenylene-bisoxy-bis(methylene)-bis(1,2,3-triazole-N-phenylacetamide) derivatives 8a–m were synthesized as potent α-glucosidase inhibitors. Compounds 8a–m were designed based on previously reported potent anti-α-glucosidase agents, and their in vitro assays against α-glucosidase demonstrated that the most potent compound among these compounds was significantly more potent than the template compounds. According to the in vitro assay, the most potent compound in this work, compound 8m, was 25 000-fold more potent than the standard inhibitor acarbose and 118.5-fold more potent than the best template used in its design. A kinetic study of compound 8m revealed that this compound is a competitive inhibitor of α-glucosidase. Molecular docking and dynamics studies were performed on this compound, which confirmed its interaction with the active site of α-glucosidase with a favorable binding energy. This journal is © The Royal Society of Chemistry, 2026.