Abstract
A new series of 2-substituted quinazolin-4(3 H )-one derivatives including coumarin nucleus has been synthesized and screened for their lipase and α-glucosidase inhibition properties. Among the synthesized compounds, N '-{2-[2-(3,4-dichlorobenzyl)-4-oxoquinazolin-3(4 H )-yl]acetyl}-2-oxo-2 H -chromene-3-carbohydrazide and N '-{2-[2-(4-bromobenzyl)-4-oxoquinazolin-3(4 H )-yl]acetyl}-2-oxo-2 H -chromene-3-carbohydrazide showed the best inhibitory effect against α-glucosidase with IC 50 values of 6.11 ± 0.40 and 7.34 ± 0.37 µM, respectively. These compounds also showed strong anti-lipase activity (IC 50 3.52 ± 0.49 and 2.85 ± 0.27 µM, respectively).
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