Momin Khan, F. Alam, M. Ateeq
Feb 16, 2022
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Abstract
Current study is focused to synthesize 4-Bromobenzohydrzide detivatives (1-29) and were examined for α-amylase enzyme inhibitory potential at various concentrations. 4-Bromobenzoic acid hydrzide detivatives (1-29) were synthesized via three stpers reaction from 4-bromobenzoic acid. Esterification was done by refluxing in MeOH for 2 hr in the presence of of concentrated H2SO4 till dissolution. In second step methyl 4-bromobenzoate and hydrazine hydrate in excess (1:5) was refluxed in methanol. 4-Bromobenzohydrazide hydrazones were synthesized by the condensation reaction of substituted aryl aldehydes and 4-bromobenzohydrazide in the presence of ethanol and glacial acetic acid. All synthesized derivatives demonstrated good inhibitory activities in the range of IC50= 0.217±0.012-5.5±0.019 as compared to standard Acarbose having IC50 = 1. 34 ± 0. 019. Out of twenty nine (29) derivatives, only five (05) compounds 23 8, 24, 9, and 13 showed less activity than the standard. Results of the enzyme inhibition its self showed that the activity of this library is due to the core structure. The slightly changes in activity is might be due to the different substitutions and position of the substitution. Furthermore; molecular docking study was performed in order to explore the possible binding mode of the synthesized compounds against α-amylase enzyme.