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

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±0.12μM); being compound 4d with the p-hydroxy phenyl motive the most active (IC50 20.24±0.72μM). Molecular modeling studies show the interactions of compound 4d with the active site of target α-glucosidase kinase.

Keywords: Acarbose; Diabetes; MMFF94X+Solvation; Pyridine-2,4,6-tricarbohydrazide; α-Glucosidase; β-Glucosidase.