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Benzoylquinazolinone derivatives 3a–n were synthesized via a simple one‐step reaction, and evaluated for in vitro α‐glucosidase inhibitory activity. Compounds 3d, 3f–g, 3i, and 3m–n showed more inhibitory activity than standard drug acarbose (IC50 = 750.0 ± 1.5 μM), and among them, compound 3d displayed the highest α‐glucosidase inhibitory activity (IC50 = 261.6 ± 0.1 μM). The kinetic analysis of...