JOURNAL 196


Organic Communications
VOLUME & ISSUE
Year: 2013 Issue: 1 January-March
PAGES
p.55 - 67
STATISTICS
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AUTHORS
    Tijen Önkol, Mehtap Gökçe, İlkay Orhan and Fatma Kaynak
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GRAPHICAL ABSTRACT


ABSTRACT


In this study eighteen new N’-[(4-Substituephenyl)sulfonyl]-2-[4-(Substituephenyl)-piperazine]-3(2H)-pyridazinone-2-yl acetohydrazide V derivatives were synthesized as acetylcholinesterase and butyrylcholinesterase inhibitors. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChe) inhibitory activity of V derivatives was measured using Ellman’s method. Some of N’-[(substituted phenyl)sulfonyl]-2-(6-substituted-3(2H)-pyridazinone-2-yl)acetohydrazides V showed inhibitory activities close galantamine at 0.05 mM 0.1 mM and 0.2 mM concentrations . According to screening data, the analog of derivatives of V which possessed CF 3 on para position of phenylsulfonyl ring improved anti-AChE activity. Also antimicrobial activity of the synthesized compounds have been evaluated. In general V Derivatives showed weak antibacterial activity when compared reference compounds. Also all the compounds are less potent than fluconazole against yeast like fungi.

KEYWORDS
  • 3(2H)-Pyridazinone
  • p-substituted sulfonylchloride acetohydrazides
  • acetylcholinesterase (AChE) inhibitor
  • butyrylcholinesterase (BChE) inhibitor.