Synthesis and biological evaluation of new benzimidazole-1,2,3-triazole hybrids as potential α-glucosidase inhibitors.

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.
PMID: 31838286 [PubMed - as supplied by publisher]

Source: Bioorganic Chemistry - December 3, 2019 Category: Chemistry Authors: Asemanipoor N, Mohammadi-Khanaposhtani M, Moradi S, Vahidi M, Asadi M, Faramarzi MA, Mahdavi M, Biglar M, Larijani B, Hamedifar H, Hajimiri MH Tags: Bioorg Chem Source Type: research