Effects of aryl methanesulfonate derivatives on acetylcholinesterase and butyrylcholinesterase

J Biochem Mol Toxicol. 2018 Nov;32(11):e22210. doi: 10.1002/jbt.22210. Epub 2018 Aug 8.

Abstract

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.

Keywords: Alzheimer's disease (AD); Ellman's method; acetylcholinesterase (AChE); aryl methanesulfonate; butyrylcholinesterase (BuChE).

Publication types

  • Comparative Study

MeSH terms

  • Acetylcholinesterase / chemistry
  • Acetylcholinesterase / metabolism
  • Animals
  • Butyrylcholinesterase / chemistry
  • Butyrylcholinesterase / metabolism
  • Cholinesterase Inhibitors / pharmacology*
  • Dithionitrobenzoic Acid / chemistry
  • Drug Discovery*
  • Electrophorus
  • Fish Proteins / antagonists & inhibitors
  • Fish Proteins / metabolism
  • Horses
  • Mesylates / pharmacology*
  • Nerve Tissue Proteins / antagonists & inhibitors
  • Nerve Tissue Proteins / metabolism
  • Nootropic Agents / pharmacology*
  • Osmolar Concentration
  • Spectrophotometry
  • Sulfhydryl Reagents / chemistry

Substances

  • Cholinesterase Inhibitors
  • Fish Proteins
  • Mesylates
  • Nerve Tissue Proteins
  • Nootropic Agents
  • Sulfhydryl Reagents
  • Dithionitrobenzoic Acid
  • Acetylcholinesterase
  • Butyrylcholinesterase