Synthesis of novel 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/-nonsubstituted benzal)hydrazone derivatives and acetylcholinesterase and butyrylcholinesterase inhibitory activities in vitro

UTKU S., Gokce M., ERDOĞAN ORHAN İ., Sahin M. F.

ARZNEIMITTELFORSCHUNG-DRUG RESEARCH, vol.61, no.1, pp.1-7, 2011 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 61 Issue: 1
  • Publication Date: 2011
  • Doi Number: 10.1055/s-0031-1296161
  • Journal Name: ARZNEIMITTELFORSCHUNG-DRUG RESEARCH
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.1-7
  • Keywords: Acetylcholinesterase inhibitors, Benzal hydrazone, Butyrylcholinesterase inhibitors, 3(2H) Pyridazinone, ALZHEIMERS-DISEASE, ANTIINFLAMMATORY ACTIVITY, 3(2H)-PYRIDAZINONE
  • Lokman Hekim University Affiliated: No

Abstract

In this study thirteen 6-substituted-3(2H)-pyridazinone-2-acety1-2-(substituted/-nonsubstituted benzal)hydrazone V derivatives were synthesized acetylcholinesterase and butyrylcholinesterase inhibitors. Ten of the synthesized compounds were synthesized for the first time in this study and the rest of them had been synthesized in a previous study. The structures of compounds V were elucidated by IR, H-1-NMR and MASS spectra. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChe) inhibitory activities of V derivatives were measured using Ellman's method. While some of the 6-substituted-3(2H)-pyridazinone-2-propyl-3-(substituted/-nonsubstituted benzal)hydrazone V derivatives exhibited significant AChE inhibitory activity, none of the compounds showed BChE inhibitory activity. These results indicate that V derivatives were AChE inhibitors with AChE/BChE selectivity.