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Triazoloquinazolines as a new class of potent α-glucosidase inhibitors: in vitro evaluation and docking study

Article scientifique 2019 Anglais

Résumé

Previously, we synthesized triazoloquinazolines 1-14 and characterized their structure. In this study, we aimed to evaluate the in vitro activity of the targets 1-14 as α-glucosidase inhibitors using α-glucosidase enzyme from Saccharomyces cerevisiae type 1. Among the tested compounds, triazoloquinazolines 14, 8, 4, 5, and 3 showed the highest inhibitory activity (IC50 = 12.70 ± 1.87, 28.54 ± 1.22, 45.65 ± 4.28, 72.28 ± 4.67, and 83.87 ± 5.12 μM, respectively) in relation to that of acarbose (IC50 = 143.54 ± 2.08 μM) as a reference drug. Triazoloquinazolines were identified herein as a new class of potent α-glucosidase inhibitors. Molecular docking results envisaged the plausible binding interaction between the target triazoloquinazolines and α-glucosidase enzyme and indicated considerable interaction with the active site residues.

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Abuelizz, H., Anouar, E., Ahmad, R., Azman, N., Marzouk, M., Al‐Salahi, R. (2019). Triazoloquinazolines as a new class of potent α-glucosidase inhibitors: in vitro evaluation and docking study. https://doi.org/10.1371/journal.pone.0220379

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Auteur(s)

Hatem A. Abuelizz El Hassane Anouar Rohaya Ahmad Nor Izzati Iwana Nor Azman Mohamed Marzouk Rashad Al‐Salahi

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