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Benzimidazole derivatives have emerged as important scaffolds in the development of potent and effective α-glucosidase inhibitors, key targets for managing type 2 diabetes mellitus (T2DM). This review highlights structural innovations and structure-activity relationships (SARs) of diverse benzimidazole-based compounds, including hybrids with Schiff bases, thiosemicarbazones, 1,2,3-triazoles, and oxadiazoles, all exhibiting α-glucosidase inhibitory activity. Notably, numerous derivatives demonstrate superior inhibition compared to the standard reference drug, acarbose.
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Shafiee et al. (2026) studied this question.
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