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Synthesis and Biological Evaluation of New Benzimidazole-1,2,3-Triazole Hybrids As Potential Α-Glucosidase Inhibitors Publisher Pubmed



Asemanipoor N1 ; Mohammadikhanaposhtani M2 ; Moradi S1 ; Vahidi M3 ; Asadi M4 ; Faramarzi MA3 ; Mahdavi M5 ; Biglar M5 ; Larijani B5 ; Hamedifar H6 ; Hajimiri MH7
Authors

Source: Bioorganic Chemistry Published:2020


Abstract

In this study, a series of benzimidazole-1,2,3-triazole hybrids 8a-n as new α-glucosidase inhibitors were designed and synthesized. In vitro α-glucosidase inhibition activity results indicated that all the synthesized compounds (IC50 values ranging from 25.2 ± 0.9 to 176.5 ± 6.7 μM) exhibited more inhibitory activity in comparison to standard drug acarbose (IC50 = 750.0 ± 12.5 μM). Enzyme kinetic study on the most potent compound 8c revealed that this compound was a competitive inhibitor into α-glucosidase. Moreover, the docking study was performed in order to evaluation of interaction modes of the synthesized compounds in the active site of α-glucosidase and to explain structure-activity relationships of the most potent compounds and their corresponding analogs. © 2019 Elsevier Inc.
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