2. Academic Validation
  3. Coumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors

Coumarin linked to 2-phenylbenzimidazole derivatives as potent α-glucosidase inhibitors

  • Sci Rep. 2024 Mar 28;14(1):7408. doi: 10.1038/s41598-024-57673-z.
Mina Sadeghi Ganjeh 1,  Ali Mazlomifar 2,  Ashraf Sadat Shahvelayti 1,  Shiva Khalili Moghaddam 3
Affiliations

Affiliations

  • 1 Department of Chemistry, College of Basic Sciences, Yadegar-e-Imam Khomeini (RAH) Shahre Rey Branch, Islamic Azad University, Tehran, Iran.
  • 2 Department of Chemistry, College of Basic Sciences, Yadegar-e-Imam Khomeini (RAH) Shahre Rey Branch, Islamic Azad University, Tehran, Iran. mazloomifar@yahoo.com.
  • 3 Department of Biology, College of Basic Sciences, Yadegar-e-Imam Khomeini (RAH) Shahre Rey Branch, Islamic Azad University, Tehran, Iran.
PMID: 38548784 DOI: 10.1038/s41598-024-57673-z
Abstract

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.

Keywords

2-Phenylbenzimidazole; Coumarin; Molecular modeling; α-Glucosidase.

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