Inhibition of acetylcholinesterase (AChE) enzyme by naphthalenylmethylen hydrazine derivative compounds

Şirinzade H.

3rd International Eurasian Conference on Science, Engineering and Technology (EurasianSciEnTech 2021) December 15-17, 2021, Ankara, Turkey, 15 - 17 December 2021, pp.123

  • Publication Type: Conference Paper / Summary Text
  • City: Ankara
  • Country: Turkey
  • Page Numbers: pp.123
  • Erzincan Binali Yildirim University Affiliated: Yes


Alzheimer's is a very common dementia disease recently and there is no definite cure. In Alzheimer's disease, which causes a decrease in neurotransmitters in the brain, the decrease in acetylcholine neurotransmitter is seen the most. To treat or prevent the disease, the degradation of acetylcholine should be reduced, and this is possible with the inhibition of acetylcholinesterase (AChE), which breaks down acetylcholine.1

To investigate the in vitro effect of naphthalenylmethylen hydrazine derivative compounds on AChE enzyme, first, pure enzyme was supplied ready. Enzyme activity was determined according to the method performed by Ellman et al.2 Acetylthiocholine iodate (AChI) was used as substrate. The yellow colored 5-thio-2-nitrobenzoate anion, which is formed because of hydrolysis of the substrates and then the reaction of DTNB with thiocholine, gives maximum absorbance at 412 nm wavelength.3

The inhibition effects of novel naphthalenylmethylen hydrazine derivative compounds (1a-1h) used in the study on the AChE enzyme were determined and the IC50 value at the nano molar level was calculated. It was observed that these compounds inhibited the enzyme significantly. In our study, IC50 values were determined to be in the range of 21.3-669.7 nM. Compared to the control compound Tacrine (IC50: 28.6 nM), 1c compound showed the best inhibitory effect.