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  • Title: Synthesis, in vitro evaluation and molecular docking studies of novel triazine-triazole derivatives as potential α-glucosidase inhibitors.
    Author: Wang G, Peng Z, Wang J, Li X, Li J.
    Journal: Eur J Med Chem; 2017 Jan 05; 125():423-429. PubMed ID: 27689725.
    Abstract:
    A novel series of triazine-triazole derivatives 7a-7m were synthesized, characterized by 1H NMR and evaluated for their α-glucosidase inhibitory activity. All the synthesized compounds displayed potent α-glucosidase inhibitory activity with IC50 range of 11.63 ± 0.15 to 37.44 ± 0.35 μM, when compared to the standard drug acarbose (IC50 = 817.38 ± 6.27 μM). Among the series, compound 7i (IC50 = 11.63 ± 0.15 μM) bearing 2,5-dichloro substitution at phenyl ring, represented the most potent α-glucosidase inhibitory activity. Molecular docking studies of the most active compounds with the homology modelled α-glucosidase were also performed to explore the possible inhibitory mechanism. Our studies shown that these triazine-triazole derivatives are a new class of α-glucosidase inhibitors.
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