N‐Substituted Arylidene‐3‐(Methylsulfonyl)‐2‐Oxoimidazolidine‐1‐Carbohydrazide as Cholinesterase Inhibitors: Design, Synthesis, and Molecular Docking Study

The development of new enzyme inhibitors in degenerative brain diseases has gained more attention. Enzyme inhibitors play an effective role in controlling central nervous system diseases. For this purpose, a novel series of hydrazone derivatives containing imidazolidine ring aimed against Alzheimer&...

Full description

Saved in:
Bibliographic Details
Published in:Chemistry & biodiversity 2022-08, Vol.19 (8), p.e202200265-n/a
Main Authors: Tok, Fatih, Sağlık, Begüm Nurpelin, Özkay, Yusuf, Kaplancıklı, Zafer Asım, Koçyiğit‐Kaymakçıoğlu, Bedia
Format: Article
Language:English
Subjects:
Acetylcholinesterase
Alzheimer's disease
Amyloid
Aromatic compounds
Attention
Biological activity
Central nervous system
Central nervous system diseases
Chemical synthesis
Cholinesterase
Cholinesterase inhibitors
Donepezil
Enzyme inhibitors
Enzymes
hydrazone
Hydrazones
imidazolidine ring
Medical treatment
Molecular docking
molecular modeling
Neurodegenerative diseases
NMR
Nuclear magnetic resonance
β-amyloid plaque
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The development of new enzyme inhibitors in degenerative brain diseases has gained more attention. Enzyme inhibitors play an effective role in controlling central nervous system diseases. For this purpose, a novel series of hydrazone derivatives containing imidazolidine ring aimed against Alzheimer's disease (AD), have been designed and synthesized. The acetylcholinesterase (AChE) enzyme inhibitory activity of these compounds was investigated. The structures of the compounds were determined by IR, 1H and 13C‐NMR and mass spectroscopic methods. Inhibition studies on the cholinesterase (ChE) enzymes and β‐amyloid plaque inhibition test of the compounds were performed. Based on the experimental results, compound 3j bearing dimethoxy substituent on the aromatic ring like donepezil exhibited the most AChE inhibitory activity with the IC50 values of 0.023±0.001 μM. Owing to obtained biological activity and molecular docking study results, it is thought that the most active compound 3j may play a role in both symptomatic and palliative treatment of AD.
ISSN:1612-1872
1612-1880
DOI:10.1002/cbdv.202200265