Synthesis, spectral characterization and α-amylase inhibition studies of Coumarin-hydrazone derivatives

A series of nineteen molecules of Coumarin hydrazone derivatives have been synthesized. The purpose of the study was to investigate the anti-diabetic activity of the synthesized Coumarin derivatives by inhibition of α-amylase. The α-amylase enzyme was isolated from the microbial source Aspergillus Niger. The experiment was conducted by taking 5, 10, 50,100 µM of each of the compounds and Acarbose was taken as a positive control. The studies showed that compoundN'-(2,4-dichlorobenzylidene)-4-((4-methyl-2-oxo-2H-chromen-7-yl)oxy)butanehydrazide (5f) (IC₅₀=114.6 µM), 4-((4-methyl-2-oxo-2H-chromen-7-yl)oxy)-N'-(4-nitrobenzylidene)butanehydrazide (5g) (IC₅₀=193.5µM), 4-((4-methyl-2-oxo-2H-chromen-7-yl)oxy)-N'-(4-methylbenzylidene)butanehydrazide(5i) (IC₅₀=128.9µM), N'-(1-(4-methoxyphenyl)ethylidene)-4-((4-methyl-2-oxo-2H-chromen-7-yl)oxy) butanehydrazide (6d)((IC₅₀=183.1µM)and N'-(1-(2,7-dichloro-8-nitroquinolin-4-yl)ethylidene)-4-((4-methyl-2-oxo-2H-chromen -7-yl)oxy)butanehydrazide (7e) (IC₅₀=110.4µM)was showing better inhibition activity against the enzyme, in comparison with the standard (IC₅₀=126.5 µM). The synthesized drug may be helpful to control the glucose level asα-amylase is one of the causes of increased sugar level in our body.