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Biscoumarin-1,2,3-Triazole Hybrids As Novel Anti-Diabetic Agents: Design, Synthesis, in Vitro Α-Glucosidase Inhibition, Kinetic, and Docking Studies Publisher Pubmed



Asgari MS1 ; Mohammadikhanaposhtani M2 ; Kiani M3 ; Ranjbar PR1 ; Zabihi E2 ; Pourbagher R2 ; Rahimi R4 ; Faramarzi MA3 ; Biglar M5 ; Larijani B5 ; Mahdavi M5 ; Hamedifar H6 ; Hajimiri MH7
Authors

Source: Bioorganic Chemistry Published:2019


Abstract

A novel series of biscoumarin-1,2,3-triazole hybrids 6a-n was prepared and evaluated for α-glucosidase inhibitory potential. All fourteen derivatives exhibited excellent α-glucosidase inhibitory activity with IC50 values ranging between 13.0 ± 1.5 and 75.5 ± 7.0 µM when compared with the acarbose as standard inhibitor (IC50 = 750.0 ± 12.0 µM). Among the synthesized compounds, compounds 6c (IC50 = 13.0 ± 1.5 µM) and 6g (IC50 = 16.4 ± 1.7 µM) exhibited the highest inhibitory activity against α-glucosidase and were non-cytotoxic towards normal fibroblast cells. Kinetic study revealed that compound 6c inhibits the α-glucosidase in a competitive mode. Furthermore, molecular docking investigation was performed to find interaction modes of the biscoumarin-1,2,3-triazole derivatives. © 2019 Elsevier Inc.
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