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, cilt.61, sa.1, ss.1-7, 2011 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 61 Sayı: 1
  • Basım Tarihi: 2011
  • Doi Numarası: 10.1055/s-0031-1296161
  • Dergi Adı: ARZNEIMITTELFORSCHUNG-DRUG RESEARCH
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.1-7
  • Anahtar Kelimeler: Acetylcholinesterase inhibitors, Benzal hydrazone, Butyrylcholinesterase inhibitors, 3(2H) Pyridazinone, ALZHEIMERS-DISEASE, ANTIINFLAMMATORY ACTIVITY, 3(2H)-PYRIDAZINONE
  • Lokman Hekim Üniversitesi Adresli: Hayır

Özet

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.