Effects of aryl methanesulfonate derivatives on acetylcholinesterase and butyrylcholinesterase

There is a dire need for new treatments for Alzheimer's disease (AD). Principal drugs have reached maturity, and the number of people affected by AD is growing at a rapid rate. After years of research and many clinical trials, only symptomatic treatments are available. An effective disease‐modi...

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Bibliographic Details
Published in:Journal of biochemical and molecular toxicology 2018-11, Vol.32 (11), p.e22210-N/A
Main Authors: Zilbeyaz, Kani, Stellenboom, Nashia, Guney, Murat, Oztekin, Aykut, Senturk, Murat
Format: Article
Language:English
Subjects:
Acetylcholinesterase
acetylcholinesterase (AChE)
Acetylcholinesterase - chemistry
Acetylcholinesterase - metabolism
Alzheimer's disease
Alzheimer's disease (AD)
Animals
Aromatic compounds
aryl methanesulfonate
butyrylcholinesterase (BuChE)
Butyrylcholinesterase - chemistry
Butyrylcholinesterase - metabolism
Cholinesterase Inhibitors - pharmacology
Clinical trials
Derivatives
Dithionitrobenzoic Acid - chemistry
Drug Discovery
Electrophorus
Ellman's method
Fish Proteins - antagonists & inhibitors
Fish Proteins - metabolism
Horses
Medical research
Medical treatment
Mesylates - pharmacology
Nerve Tissue Proteins - antagonists & inhibitors
Nerve Tissue Proteins - metabolism
Neurodegenerative diseases
Nootropic Agents - pharmacology
Osmolar Concentration
Spectrophotometry
Sulfhydryl Reagents - chemistry
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Summary:There is a dire need for new treatments for Alzheimer's disease (AD). Principal drugs have reached maturity, and the number of people affected by AD is growing at a rapid rate. After years of research and many clinical trials, only symptomatic treatments are available. An effective disease‐modifying drug for AD needs to be discovered. The research presented in this paper aims to facilitate in the discovery of new potential targets that could help in the ongoing AD research. Aryl methanesulfonate derivatives were screened for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities. IC50 values between 0.660 and 3.397 µM against AChE and 0.885 and 2.596 µM against BuChE were obtained.
ISSN:1095-6670
1099-0461
DOI:10.1002/jbt.22210