Synthesis, Molecular Docking Studies and Biological Evaluation o f 3-Iminoaurones as Acetylcholinesterase and Butyrylcholinesterase Inhibitors

Author(s): Ehsan Ullah Mughal*, Amina Sadiq, Bilal Ahmad Khan, Muhammad Naveed Zafar, Ishtiaq Ahmed, Muhammad Zubair

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 9 , 2017

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Graphical Abstract:


Background: A new series of aurone-hydrazones have been designed and synthesized in order to explore new bioactive compounds, which could have potential to be used as active drugs against Alzheimer’s disease.

Methods: The newly synthesized compounds were characterized by various spectroscopic techniques (IR, mass spectrometry and NMR spectroscopy) and evaluated in vitro for their inhibitory potential against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. All target compounds exhibited varied degree of IC50 values compared to standard Donepezil. Among the series, the compound 6c was found as a potent dual inhibitor of AChE and BChE having IC50values 0.92±0.01 and 2.25±0.01 μM respectively.

Results and Conclusion: The experimental results were further supported by molecular docking analysis. Both studies showed that some of these compounds are interesting inhibitors against AChE and BChE enzymes.

Keywords: Alzheimer’s disease, aurones, 3-iminoaurones, 2, 4-dinitrophenyl hydrazones, molecular docking analysis, acetylcholinesterase, butyrylcholinesterase.

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Article Details

Year: 2017
Page: [1035 - 1041]
Pages: 7
DOI: 10.2174/1570180814666170106123959
Price: $65

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