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Design, synthesis and anticholinesterase activity of a novel series of 1-benzyl-4-((6-alkoxy-3-oxobenzofuran-2(3H)-ylidene) methyl) pyridinium derivatives.

Bioorganic & medicinal chemistry 2010 Jul 28; In press

Link to PubMed abstract

Nadri H, Pirali-Hamedani M, Shekarchi M, Abdollahi M, Sheibani V, Amanlou M, Shafiee A, Foroumadi A

Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran.

A novel series of benzofuranone-ylidene-methyl benzylpyridinium derivatives (6a-u) were synthesized as acetylcholinesterase inhibitors. The anticholinesterase activity of synthesized compounds was measured using colorimetric Ellman's method. It was revealed that some synthesized compounds exhibited high anticholinesterase activity, among them compound 6b was the most active compound (IC(50)=10+/-6.87nM).

Keywords: acetylcholinesterase