Submit Manuscript  

Article Details


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

[ Vol. 14 , Issue. 9 ]

Author(s):

Ehsan Ullah Mughal, Amina Sadiq, Bilal Ahmad Khan, Muhammad Naveed Zafar, Ishtiaq Ahmed and Muhammad Zubair   Pages 1035 - 1041 ( 7 )

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.

Affiliation:

Department of Chemistry, University of Gujrat, Gujrat 50700, Department of Chemistry, Govt. College Women University, Sialkot 51300, Department of Chemistry, University of Azad Jammu and Kashmir, Muzaffarabad, Department of Chemistry, Quaid-i-Azam University, Islamabad-45320, Karlsruhe Institute of Technology (KIT), Institute for Biological Interfaces (IBG-1), Hermann-von-Helmholtz-Platz, D-76344 Eggenstein-Leopoldshafen, Department of Chemistry, University of Gujrat, Gujrat 50700

Graphical Abstract:



Read Full-Text article