biostudies-literatureUnknown14(1)Ganjeh MSα-Glucosidase inhibitors have emerged as crucial agents in the management of type 2 diabetes mellitus. In the present study, a new series of coumarin-linked 2-phenylbenzimidazole derivatives 5a-m was designed, synthesized, and evaluated as anti-α-glucosidase agents. Among these derivatives, compound 5k (IC₅₀ = 10.8 µM) exhibited a significant inhibitory activity in comparison to the positive control acarbose (IC₅₀ = 750.0 µM). Through kinetic analysis, it was revealed that compound 5k exhibited a competitive inhibition pattern against α-glucosidase. To gain insights into the interactions between the title compounds and α-glucosidase molecular docking was employed. The obtained results highlighted crucial interactions that contribute to the inhibitory activities of the compounds against α-glucosidase. These derivatives show immense potential as promising starting points for developing novel α-glucosidase inhibitors.Scientific reports7408https://www.ebi.ac.uk/biostudies/studies/S-EPMC10978946biostudies-literatureCoumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors.PMC10978946Mazlomifar AGanjeh MSShahvelayti ASMoghaddam SKfalseCoumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors.α-Glucosidase inhibitors have emerged as crucial agents in the management of type 2 diabetes mellitus. In the present study, a new series of coumarin-linked 2-phenylbenzimidazole derivatives 5a-m was designed, synthesized, and evaluated as anti-α-glucosidase agents. Among these derivatives, compound 5k (IC₅₀ = 10.8 µM) exhibited a significant inhibitory activity in comparison to the positive control acarbose (IC₅₀ = 750.0 µM). Through kinetic analysis, it was revealed that compound 5k exhibited a competitive inhibition pattern against α-glucosidase. To gain insights into the interactions between the title compounds and α-glucosidase molecular docking was employed. The obtained results highlighted crucial interactions that contribute to the inhibitory activities of the compounds against α-glucosidase. These derivatives show immense potential as promising starting points for developing novel α-glucosidase inhibitors.2024-01-01T00:00:00Z2024 Mar2025-04-26T11:24:59.365Z2025-04-06T13:42:16.173ZS-EPMC109789463854878410.1038/s41598-024-57673-z