Synthesis, Enzyme Inhibition, and Molecular Docking Studies of Hydrazones from Dichlorophenylacetic Acids

2016 
A series of hydrazones 5a–i were synthesized by the condensation of hydrazides derived from dichlorophenylacetic acids with different aromatic aldehydes and ketones. Their structures were confirmed by spectroscopic data and elemental analysis. Hydrazones 5a–i were evaluated for α-glucosidase and urease inhibition activities. Five compounds exhibited potent α-glucosidase inhibitory potential with IC50 values 8.5 ± 0.3, 22.2 ± 0.78, 32.9 ± 1.5, 34 ± 2.4, and 170.6 ± 7.5 μM, respectively, which are many times better than that of the standard inhibitor acarbose (IC50  = 840 ± 1.73 μM). Furthermore, molecular docking study was performed to explore the binding mode in the active sites of α-glucosidase and urease enzymes.
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