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

Authors

  • Emre Menteşe Department of Chemistry, Faculty of Art and Sciences, Recep Tayyip Erdogan University, Fener St., 53100 Rize
  • Nesrin Karaali Department of Chemistry, Faculty of Art and Sciences, Recep Tayyip Erdogan University, Fener St., 53100 Rize
  • Gülay Akyüz Department of Chemistry, Faculty of Art and Sciences, Recep Tayyip Erdogan University, Fener St., 53100 Rize
  • Fatih Yılmaz Department of Chemistry, Faculty of Art and Sciences, Recep Tayyip Erdogan University, Fener St., 53100 Rize
  • Serdar Ülker Department of Biology, Faculty of Art and Sciences, Recep Tayyip Erdogan University, Fener St., 53100 Rize
  • Bahittin Kahveci Department of Nutrition and Dietetics, Faculty of Health Sciences, Karadeniz Technical University, Farabi St., 61080 Trabzon

DOI:

https://doi.org/10.1007/3367

Keywords:

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

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).

Author Biographies

Emre Menteşe, Department of Chemistry, Faculty of Art and Sciences, Recep Tayyip Erdogan University, Fener St., 53100 Rize

Nesrin Karaali, Department of Chemistry, Faculty of Art and Sciences, Recep Tayyip Erdogan University, Fener St., 53100 Rize

Gülay Akyüz, Department of Chemistry, Faculty of Art and Sciences, Recep Tayyip Erdogan University, Fener St., 53100 Rize

Fatih Yılmaz, Department of Chemistry, Faculty of Art and Sciences, Recep Tayyip Erdogan University, Fener St., 53100 Rize

Serdar Ülker, Department of Biology, Faculty of Art and Sciences, Recep Tayyip Erdogan University, Fener St., 53100 Rize

Bahittin Kahveci, Department of Nutrition and Dietetics, Faculty of Health Sciences, Karadeniz Technical University, Farabi St., 61080 Trabzon

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Published

2017-01-06

Issue

Vol. 52 No. 12 (2016)

Section

Original Papers