| Literature DB >> 31679980 |
Mina Saeedi1, Maryam Mohammadi-Khanaposhtani2, Mohammad Sadegh Asgari3, Nafiseh Eghbalnejad4, Somaye Imanparast5, Mohammad Ali Faramarzi5, Bagher Larijani6, Mohammad Mahdavi7, Tahmineh Akbarzadeh8.
Abstract
In this work, new derivatives of diarylimidazole-1,2,3-triazole 7a-p were designed, synthesized, and evaluated for their in vitro α-glucosidase inhibitory activity. All compounds showed potent inhibitory activity in the range of IC50 = 90.4-246.7 µM comparing with acarbose as the standard drug (IC50 = 750.0 µM). Among the synthesized compounds, compounds 7b, 7c, and 7e were approximately 8 times more potent than acarbose. The kinetic study of those compounds indicated that they acted as the competitive inhibitors of α-glucosidase. Molecular docking studies were also carried out for compounds 7b, 7c, and 7e using modeled α-glucosidase to find the interaction modes responsible for the desired inhibitory activity.Entities:
Keywords: 1,2,3-triazole; Diarylimidazole; Docking study; Kinetic study; α-Glucosidase inhibitors
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Year: 2019 PMID: 31679980 DOI: 10.1016/j.bmc.2019.115148
Source DB: PubMed Journal: Bioorg Med Chem ISSN: 0968-0896 Impact factor: 3.641