Title:Design, Synthesis and Acetylcholinesterase and Butylcholinesterase Inhibition Activity of Novel 1-(Alkyl)-3-(2-oxo-2H-chromenyloxy Acetamido) methylpyridinium Salts
Volume: 18
Issue: 7
Author(s): Mehri Abdollahi fard, Mohammadreza Manafi*, Manijeh Motevalian and Seyed Saied Homami
Affiliation:
- Department of Applied Chemistry, Faculty of Science, South Tehran Branch, Islamic Azad University, Tehran,Iran
Keywords:
Coumarin, synthesis, Alzheimer's disease, enzyme inhibition, AChE inhibition, BuChe inhibition.
Abstract: In this paper, a novel series of 1-(alkyl)-3-(2-oxo-2H-chromenyloxy acetamido) methylpyridinium
salts were synthesized in a simple and efficient way. The method showed to be facile and the
compounds were obtained in high isolated yields. All the synthesized compounds were characterized
by 1H NMR, 13C NMR, FT-IR, Mass and elemental analysis. AChE and BuChE inhibition activity of
the synthesized compounds were evaluated and the results showed that all the compounds were active
in the inhibition of the mentioned enzymes. All the compounds were active in the inhibition of the two
studied enzymes. Among all the compounds, the compound 6a (1.85 μM) and 6i (0.106 μM) showed
the highest inhibition activity against AChE and BuChE, respectively. The kinetic study was performed
to get more insight into the mechanism of action of the synthesized compounds. Docking studies were
also performed to obtain the interactions between the synthesized compounds and the enzymes.