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

Ehsan   Ullah   Mughal; Amina      Sadiq; Bilal   Ahmad   Khan; Muhammad   Naveed   Zafar; Ishtiaq      Ahmed; Muhammad      Zubair

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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DOI https://dx.doi.org/10.2174/1570180814666170106123959	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X

Letters in Drug Design & Discovery

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

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