Novel pyridine-2,4,6-tricarbohydrazide derivatives: Design, synthesis, characterization and in vitro biological evaluation as α- And β-glucosidase inhibitors

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Abstract

A range of novel pyridine 2,4,6-tricarbohydrazide derivatives (4a-4h) were synthesized and its biological inhibition towards α- and β-glucosidases was studied. Most of the compounds demonstrate to be active against α-glucosidase, and quite inactive/completely inactive against β-glucosidase. A number of compounds were found to be more active against α-glucosidase than the reference compound acarbose (IC50 38.25 ± 0.12 μM); being compound 4d with the p-hydroxy phenyl motive the most active (IC50 20.24 ± 0.72 μM). Molecular modeling studies show the interactions of compound 4d with the active site of target α-glucosidase kinase.

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Riaz, S., Khan, I. U., Yar, M., Ashraf, M., Rehman, T. U., Shaukat, A., … Alves, M. J. (2014). Novel pyridine-2,4,6-tricarbohydrazide derivatives: Design, synthesis, characterization and in vitro biological evaluation as α- And β-glucosidase inhibitors. Bioorganic Chemistry, 57, 148–154. https://doi.org/10.1016/j.bioorg.2014.10.007

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