Tehran University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! On (X network) By
Benzoylquinazolinone Derivatives As New Potential Antidiabetic Agents: Α-Glucosidase Inhibition, Kinetic, and Docking Studies Publisher



Mohammadikhanaposhtani M1 ; Yahyavi H2 ; Imanparast S3 ; Harandi FN4 ; Faramarzi MA3 ; Foroumadi A2 ; Larijani B5 ; Biglar M5 ; Mahdavi M5
Authors
Show Affiliations
Authors Affiliations
  1. 1. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
  2. 2. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Biotechnology Group, Chemical Engineering Department, Tarbiat Modares University, Tehran, Iran
  5. 5. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran

Source: Journal of the Chinese Chemical Society Published:2020


Abstract

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 the compound 3d revealed that this compound inhibited α-glucosidase in a competitive manner (Ki = 255 μM). The docking studies were applied to predict binding modes of the synthesized compounds in active site of α-glucosidase. © 2019 The Chemical Society Located in Taipei & Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim