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Design and Synthesis of Phenoxymethybenzoimidazole Incorporating Different Aryl Thiazole-Triazole Acetamide Derivatives As Α-Glycosidase Inhibitors Publisher Pubmed



Nasli Esfahani A1 ; Iraji A2, 3 ; Alamir A1 ; Moradi S1 ; Asgari MS4 ; Hosseini S5 ; Mojtabavi S6 ; Nasliesfahani E7 ; Faramarzi MA6 ; Bandarian F7 ; Larijani B8 ; Hamedifar H9 ; Hajimiri MH10 ; Mahdavi M8
Authors

Source: Molecular Diversity Published:2022


Abstract

A novel series of phenoxymethybenzoimidazole derivatives (9a-n) were rationally designed, synthesized, and evaluated for their α-glycosidase inhibitory activity. All tested compounds displayed promising α-glycosidase inhibitory potential with IC50 values in the range of 6.31 to 49.89 μM compared to standard drug acarbose (IC50 = 750.0 ± 10.0 μM). Enzyme kinetic studies on 9c, 9g, and 9m as the most potent compounds revealed that these compounds were uncompetitive inhibitors into α-glycosidase. Docking studies confirmed the important role of benzoimidazole and triazole rings of the synthesized compounds to fit properly into the α-glycosidase active site. This study showed that this scaffold can be considered as a highly potent α-glycosidase inhibitor. © 2021, The Author(s), under exclusive licence to Springer Nature Switzerland AG.
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