Drug Res (Stuttg) 2013; 63(03): 137-144
DOI: 10.1055/s-0033-1333735
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Synthesis and Biological Activity of New Donepezil-Hydrazinonicotinamide Hybrids

E. Żurek
1   Department of Pharmaceutical Chemistry and Drug Analyses, Medical University, Lodz, Poland
P. Szymański
1   Department of Pharmaceutical Chemistry and Drug Analyses, Medical University, Lodz, Poland
E. Mikiciuk-Olasik
1   Department of Pharmaceutical Chemistry and Drug Analyses, Medical University, Lodz, Poland
› Author Affiliations
Further Information

Publication History

received 11 September 2012

accepted 15 January 2013

Publication Date:
14 February 2013 (online)


Currently available treatment used in Alzheimer’s disease is based on acetylcholinesterase inhibitors, e. g. donepezil, tacrine, galantamine, and rivastigmine. In the present study some derivatives of donepezil were synthesized, and their potential anticholinesterase properties were investigated using the colorimetric Ellman’s method. These compounds were synthesized by condensation between indanone derivatives and the hydrazine nicotinated moiety (Hynic). For received derivatives, the selectivity and the IC50 values for acetylcholinesterase and butyrylcholinesterase were calculated. All the tested compounds exhibited lower affinity for AChE than donepezil and higher affinity for BChE than donepezil. Compound 33 showed the most selectivity for AChE among the obtained indanone derivatives.

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