Hetarylcoumarins: Synthesis and biological evaluation as potent α-glucosidase inhibitors

Abstract

In search of better α-glucosidase inhibitors, a series of novel hetarylcoumarins (3a-3j) were designed and synthesized through a facile multicomponent route where p-toluenesulfonic acid (PTSA) was explored as an efficient catalyst. These new scaffolds were further evaluated for their α-glucosidase inhibition potentials. All the derivatives exhibited good to excellent results which were comparable or even better than of standard drug acarbose. Of these compounds, a dihalogenated compound 3f was found to be the most effective one with IC₅₀: 2.53±0.002µM. Molecular docking has predicted the plausible binding interactions of compounds 3f, 3g and 3j with α-glucosidase.

Keywords: Antidiabetic agents; Coumarin; Imidazole; Molecular docking; α-Glucosidase inhibitors.