Abstract
In the course of studies directed towards the synthesis of novel AChE and BChE inhibitors, for the treatment of Alzheimer disease, we focused on the conventional versus microwave assisted synthesis of seventeen benzohydrazide derivatives and tested their ability as AChE and BChE inhibitors. These derivatives were characterized by FT-IR, 1H-NMR, 13C-NMR and EI-MS. Seventeen derivatives exhibited varied acetylcholinesterase inhibition with IC50 values ranging between 72.04 ± 1.12 to 1320.65 ± 0.95 μM as well as butyrylcholinesterase activity with IC50 values ranging between 3.04 ± 1.48-1876.17 ± 0.95 μM as compared with standard eserine (IC50=0.85 ± 0.0001 μM). Only two analogs 3k and 3o exhibited moderate acetylcholinesterase inhibitor potential with IC50 values 72.04 ± 1.12 and 94.06 ± 1.17 μM respectively. Five analogs 3d, 3h, 3q, 3o and 3l exhibited good potent butyrylcholinesterase inhibitory potential with IC50 values 3.04 ± 1.48, 9.01 ± 0.58, 15.12 ± 0.66, 45.00 ± 0.99 and 50.19 ± 0.62 μM respectively. Molecular docking studies were carried out in order to find out the binding affinity of benzohydrazide derivatives with the enzyme.
Highlights
Microwave irradiation has been effectively utilized as a nonconventional energy source in organic chemistry [1]
On completion of reaction, the mixture was cooled and the solvent was evaporated under reduced pressure to obtain the desired products which were washed with DCM (25 ml) and dried
The structures were determined by using spectroscopic techniques such as FTIR, 1HNMR, 13C NMR and Electron ionization (EI)-mass spectra (MS) spectroscopy
Summary
Microwave irradiation has been effectively utilized as a nonconventional energy source in organic chemistry [1]. Energy is transferred from the surfaces of the material due to thermal gradients. Microwave heating rather than heat transfer is the conversion of highly polarizing electromagnetic radiation to thermal energy which is delivered directly to materials through molecular interaction with the electromagnetic field. A number of reactions that do not occur by conventional heating can be accomplished using microwaves [2]. A great deal of literature has been found on the application of microwaves to heterocyclic chemistry [3], fullerene chemistry [4], cycloaddition reactions [5], polymers [6], homogeneous [7] and heterogeneous catalysis [8], green chemistry [9] and many more
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