Design, Synthesis and Evaluation of Some Novel 3 (2H) -Pyridazinone-2-yl-Acetohydrazides/
propionohydrazides as Acetylcholinesterase and Butyrylcholinesterase Inhibitors
A. Berna ÖZÇELİK*°, Mehtap GÖKÇE* İlkay ORHAN**, Sezer ŞENOL**

* Gazi University, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara, Turkey
** Gazi University, Department of Pharmacognosy, Faculty of Pharmacy, Ankara, Turkey
° Corresponding Author E-mail: brndemirci@yahoo.com

Summary

In order to identify new candidates that may be of value in designing acetylcholinesterase and butyrylcholinesterase inhibitors, we report herein the synthesis of some N’-[(4-Substituedphenyl) sulphonyl] -2- [4- (Substituephenyl)
-piperazine] -3 (2H) -pyridazinone-2-yl acetohydrazide/propionohydrazide V derivatives. The in vitro inhibition of AChE and BChE for the synthesized title compounds was determined by the method of Ellman et al. using galantamine as a reference. Some of V derivatives showed inhibitory activities close to galantamine at 25 μg/ml, 50 μg/ml, 100 μg/ml, 200 μg/ml concentrations. According to screening data, especially the analogues of N’- [(4-Substituedphenyl) sulphonyl] -2- [4- (substituedphenyl) -piperidine/piperazine]-3 (2H) -pyridazinone-2-yl acetohydrazide/ propionohydrazide V, which possessed CF3 on para position of phenylsulfonyl ring improved anti-AChE activity.

Key Words :
Pyridazinones, Acetohydrazides, Acetylcholinesterase, Butyrylcholinesterase.