Abstract
Thiourea derivatives having benzimidazole 1–17 have been synthesized, characterized and evaluated for α-glucosidase inhibition.
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•Thiourea derivatives having benzimidazole 1–17.•In vitro α-glucosidase inhibitory activity.•Identification of a new class of α-glucosidase inhibitors.•Molecular docking.
Thiourea derivatives having benzimidazole 1–17 have been synthesized, characterized by 1H NMR, 13C NMR and EI-MS and evaluated for α-glucosidase inhibition. Identification of potential α-glucosidase inhibitors were done by in vitro screening of 17 thiourea bearing benzimidazole derivatives using Baker’s yeast α-glucosidase enzyme. Compounds 1–17 exhibited a varying degree of α-glucosidase inhibitory activity with IC50 values between 35.83±0.66 and 297.99±1.20μM which are more better than the standard acarbose (IC50=774.5±1.94μM). Compound 10 and 14 showed significant inhibitory effects with IC50 value 50.57±0.81 and 35.83±0.66μM, respectively better than the rest of the series. Structure activity relationships were established. Molecular docking studies were performed to understand the binding interaction of the compounds.