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Aryl-Quinoline-4-Carbonyl Hydrazone Bearing Different 2-Methoxyphenoxyacetamides As Potent Α-Glucosidase Inhibitors; Molecular Dynamics, Kinetic and Structure–Activity Relationship Studies Publisher Pubmed

Summary: Can new compounds control diabetes? A study found aryl-quinoline derivatives strongly inhibit α-glucosidase, offering potential new treatments for type 2 diabetes. #DiabetesResearch #DrugDevelopment

Hamedifar H1, 2 ; Mirfattahi M3 ; Khalili Ghomi M3 ; Azizian H4 ; Iraji A5, 6 ; Noori M7 ; Moazzam A3 ; Dastyafteh N7 ; Nokhbehzaim A8 ; Mehrpour K5, 6 ; Javanshir S7 ; Mojtabavi S9 ; Faramarzi MA9 ; Larijani B3 Show All Authors
Authors
  1. Hamedifar H1, 2
  2. Mirfattahi M3
  3. Khalili Ghomi M3
  4. Azizian H4
  5. Iraji A5, 6
  6. Noori M7
  7. Moazzam A3
  8. Dastyafteh N7
  9. Nokhbehzaim A8
  10. Mehrpour K5, 6
  11. Javanshir S7
  12. Mojtabavi S9
  13. Faramarzi MA9
  14. Larijani B3
  15. Hajimiri MH10
  16. Mahdavi M3

Source: Scientific Reports Published:2024


Abstract

Regarding the important role of α-glucosidase enzyme in the management of type 2 diabetes mellitus, the current study was established to design and synthesize aryl-quinoline-4-carbonyl hydrazone bearing different 2-methoxyphenoxyacetamide (11a–o) and the structure of all derivatives was confirmed through various techniques including IR, 1H-NMR, 13C-NMR and elemental analysis. Next, the α-glucosidase inhibitory potentials of all derivatives were evaluated, and all compounds displayed potent inhibition with IC50 values in the range of 26.0 ± 0.8–459.8 ± 1.5 µM as compared to acarbose used as control, except 11f and 11l. Additionally, in silico-induced fit docking and molecular dynamics studies were performed to further investigate the interaction, orientation, and conformation of the newly synthesized compounds over the active site of α-glucosidase. © 2024, The Author(s).
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