Tehran University of Medical Sciences

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Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors Publisher Pubmed



Saeedi M1, 2 ; Mohammadikhanaposhtani M3 ; Asgari MS4 ; Eghbalnejad N5 ; Imanparast S6 ; Faramarzi MA6 ; Larijani B7 ; Mahdavi M7 ; Akbarzadeh T2, 8
Authors

Source: Bioorganic and Medicinal Chemistry Published:2019


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. © 2019 Elsevier Ltd
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