Synthesis, in
vitro and in silico evaluation of sulfonylurea-chalcone hybrid analogues as α-glucosidase
inhibitors
Wong Yee Hua, Ng Jia Jing, Wai Wan, Chee Xuan Xuan and Avupati Vasudeva Rao
Res. J. Biotech.; Vol. 20(3); 213-221;
doi: https://doi.org/10.25303/203rjbt2130221; (2025)
Abstract
Identification of novel α-glucosidase inhibitors is in urgent demand due to the
high prevalence and limitations of existing drugs used in the therapeutic management
of type 2 diabetes. In line with the need, we synthesised and evaluated a series
of sulfonylurea-chalcone hybrid analogues for their bioactive potential as α-glucosidase
inhibitors. Based on the in vitro analysis of screening results and structure-activity
relationship (SAR), compound c was found to be a promising bioactive hit molecule
(IC50: 1.776 μM).
In silico molecular docking studies revealed that the sulfonylurea-chalcone hybrid
backbone exhibited stable binding properties at the human α-glucosidase (PDB ID:
3TOP) binding site region.
