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SYNTHESIS AND EVALUATION OF α-GLUCOSIDASE AND PANCREATIC LIPASE INHIBITION BY QUINAZOLINONE-COUMARIN HYBRIDS

Emre Menteşe, Nesrin Karaali, Gülay Akyüz, Fatih Yılmaz, Serdar Ülker, Bahittin Kahveci
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Abstract


A new series of 2-substituted quinazolin-4(3H)-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(4H)-yl]acetyl}-2-oxo-2H-chromene-3-carbohydrazide and N'-{2-[2-(4-bromobenzyl)-4-oxoquinazolin-3(4H)-yl]acetyl}-2-oxo-2H-chromene-3-carbohydrazide showed the best inhibitory effect against α-glucosidase with IC50 values of 6.11 ± 0.40 and 7.34 ± 0.37 µM, respectively. These compounds also showed strong anti-lipase activity (IC50 3.52 ± 0.49 and 2.85 ± 0.27 µM, respectively).


Keywords


coumarins; quinazolin-4(3H)-one; anti-lipase activity; α-glucosidase inhibition; microwave; ultrasonication

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