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

• A series of novel pyridine 2,4,6-tricarbohydrazide derivatives are synthesized.
• This simple synthetic strategy afforded the targeted compounds in good to excellent yields.
• Most of the synthesized compounds have exhibited potent α-glucosidase activity.
• Generally hydroxyl substituted compounds showed more promising inhibition.
• Compound 4d presented the highest inhibitory activity with IC50 value 20.24 ± 0.72 μM.

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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