Design and synthesis of novel quinazolinone-1,2,3-triazole hybrids as new anti-diabetic agents: In vitro α-glucosidase inhibition, kinetic, and docking study

Oct 27, 2018Bioorganic chemistry

Design of new quinazolinone-triazole compounds as potential anti-diabetic agents with lab tests on enzyme inhibition and molecular binding

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Abstract

All synthesized quinazolinone-1,2,3-triazole hybrids exhibited inhibitory activity against yeast α-glucosidase with IC values ranging from 181.0-474.5 µM.

  • Compounds 10g and 10p showed the highest inhibitory activity against α-glucosidase among the tested hybrids.
  • Compound 10g inhibited α-glucosidase in a competitive manner with a K value of 117 µM.
  • In silico docking studies suggested specific binding modes for the most potent compounds in the α-glucosidase active site.
  • Compounds 10g and 10p demonstrated a lack of cytotoxicity in MTT assays.

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