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Synthesis, Α-Glucosidase Inhibitory Activity, and Molecular Dynamic Simulation of 6-Chloro-2-Methoxyacridine Linked to Triazole Derivatives Publisher Pubmed



Asadi M1, 2 ; Ahangari MM3 ; Iraji A4, 5 ; Azizian H1, 2 ; Nokhbehzaim A6 ; Bahadorikhalili S7 ; Mojtabavi S8 ; Faramarzi MA8 ; Nasliesfahani E9 ; Larijani B10 ; Mahdavi M10 ; Amanlou M3, 11
Authors

Source: Scientific Reports Published:2024


Abstract

Α-glucosidase inhibition can be useful in the management of carbohydrate-related diseases, especially type 2 diabetes mellitus. Therefore, in this study, a new series of 6-chloro-2-methoxyacridine bearing different aryl triazole derivatives were designed, synthesized, and evaluated as potent α-glucosidase inhibitors. The most potent derivative in this group was 7h bearing para-fluorine with IC50 values of 98.0 ± 0.3 µM compared with standard drug acarbose (IC50 value = 750.0 ± 10.5 μM). A kinetic study of compound 7h revealed that it is a competitive inhibitor against α-glucosidase. Molecular dynamic simulations of the most potent derivative were also executed and indicated suitable interactions with residues of the enzyme which rationalized the in vitro results. © The Author(s) 2024.
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