Tehran University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! 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

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
Related Docs
View other Related Docs
1. Synthesis and Structure–Activity Relationship Studies of Benzimidazole-Thioquinoline Derivatives As Α-Glucosidase Inhibitors, Scientific Reports (2023)
2. Synthesis and Biological Evaluation of New Benzimidazole-1,2,3-Triazole Hybrids As Potential Α-Glucosidase Inhibitors, Bioorganic Chemistry (2020)
3. Alpha- Glucosidase Inhibition Analysis and in Silico Studies of New Tetrahydroquinazolin-4(1H)-One Derivatives, Results in Chemistry (2024)
Experts (# of related papers)
View all Related Experts
Mohammad Ali Faramarzi (19)
Mohammad Mahdavi (15)
Other Related Docs
4. Design and Synthesis of Novel Pyrazole-Phenyl Semicarbazone Derivatives As Potential Α-Glucosidase Inhibitor: Kinetics and Molecular Dynamics Simulation Study, International Journal of Biological Macromolecules (2021)
5. Synthesis and Biological Evaluation of a New Series of Benzofuran-1,3,4-Oxadiazole Containing 1,2,3-Triazole-Acetamides As Potential Α-Glucosidase Inhibitors, Journal of Biochemical and Molecular Toxicology (2021)
6. Quinazolinone-1,2,3-Triazole-Acetamide Conjugates As Potent Α-Glucosidase Inhibitors: Synthesis, Enzyme Inhibition, Kinetic Analysis, and Molecular Docking Study, RSC Medicinal Chemistry (2023)
7. Imidazo[1,2-C]Quinazolines As a Novel and Potent Scaffold of Α-Glucosidase Inhibitors: Design, Synthesis, Biological Evaluations, and in Silico Studies, Scientific Reports (2023)
8. Pyrano[3,2-C]Quinoline Derivatives As New Class of Α-Glucosidase Inhibitors to Treat Type 2 Diabetes: Synthesis, in Vitro Biological Evaluation and Kinetic Study, Medicinal Chemistry (2019)
9. Novel N′-Substituted Benzylidene Benzohydrazides Linked to 1,2,3-Triazoles: Potent Α-Glucosidase Inhibitors, Scientific Reports (2023)
10. Design, Synthesis, Molecular Docking, and in Vitro Α-Glucosidase Inhibitory Activities of Novel 3-Amino-2,4-Diarylbenzo[4,5]Imidazo[1,2-A]Pyrimidines Against Yeast and Rat Α-Glucosidase, Scientific Reports (2021)
11. Design, Synthesis, and Molecular Docking Studies of Diphenylquinoxaline-6-Carbohydrazide Hybrids As Potent Α-Glucosidase Inhibitors, BMC Chemistry (2022)
12. Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors, Bioorganic and Medicinal Chemistry (2019)
13. Synthesis, in Vitro Evaluation, and Molecular Docking Studies of Novel Hydrazineylideneindolinone Linked to Phenoxymethyl-1,2,3-Triazole Derivatives As Potential Α-Glucosidase Inhibitors, Bioorganic Chemistry (2021)
14. 1-Phenyl-Β-Carboline-3-Carboxamide-1,2,3-Triazole-N-Phenylacetamide Hybrids As New Α-Glucosidase Inhibitors, Scientific Reports (2025)
15. Novel Pyrano[3,2-C]Quinoline-1,2,3-Triazole Hybrids As Potential Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and Molecular Dynamics Simulation, ACS Omega (2023)
16. Substituted Piperazine Conjugated to Quinoline-Thiosemicarbazide As Potent Α-Glucosidase Inhibitors to Target Hyperglycemia, Scientific Reports (2025)
17. Design, Synthesis and in Vitro Α-Glucosidase Inhibition of Novel Coumarin-Pyridines As Potent Antidiabetic Agents, New Journal of Chemistry (2018)
18. Synthesis, in Vitro and in Silico Enzymatic Inhibition Assays, and Toxicity Evaluations of New 4,5-Diphenylimidazole-N-Phenylacetamide Derivatives As Potent Α-Glucosidase Inhibitors, Medicinal Chemistry Research (2021)
19. Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies, Bioorganic and Medicinal Chemistry Letters (2019)
20. Novel Resorcinol-Based 2-Amino-4H-Chromene-3-Carbonitrile Derivatives As Α-Glucosidase Inhibitors: Synthesis, in Vitro Evaluation, and Molecular Dynamics Simulation Studies, Asian Journal of Organic Chemistry (2025)