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FABAD  J. Pharm. Sci.
ISSN 1300-4182
Copyright Ó 2010 FABAD. All rights reserved 

FABAD J. Pharm. Sci., 35(3), 153-161, 2010. PDF (594 KB)

Scientific Review

ABSTRACT

Synthesis and Acetylcholinesterase/Butyrylcholinesterase Inhibitory Activities of (Substituted/
Nonsubstituted Benzal) Hydrazone Derivatives of 3- (6-Substituted-3 (2H) - Pyridazinon-2-yl)
propionohydrazides

A. Berna ÖZÇELİK*, Mehtap GÖKÇE*°, İlkay ORHAN**, M.Fethi ŞAHİN*


* 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: mgokce@gazi.edu.tr


Summary


In this study thirteen new substituted/nonsubstituted benzalhydrazone V derivatives of 3-(6-substituted-3(2H)-pyridazinon-2-yl)propionohydrazide derivatives IV were synthesized as acetylcholinesterase and butyrylcholinesterase inhibitors. The structures of compounds V were elucidated by IR, 1H-NMR and MASS spectra. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChe) inhibitory activity of V derivatives was measured using Ellman’s method. Only (4-chlorophenylbenzal)hydrazone derivatives of 3-(6-(4-fluorophenyl)-3(2H)-pyridazinon-2-yl)propionohydrazide Vi showed an excellent inhibitory effect against AChE. In addition, Vi showed a significant inhibitory effect against BChE.

Key Words :
Pyridazinone, Benzalhydrazone, AChE inhibitory, BChe inhibitory.