title: Synthesis and biological activity of new donepezil-hydrazinonicotinamide hybrids.
abstract: 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.
authors: Department of Pharmaceutical Chemistry and Drug Analyses, Medical University, Lodz, Poland. elzbieta.zurek@umed.lodz.pl
authors: E
authors: E
authors: Zurek
authors: P
authors: P
authors: Szymański
authors: E
authors: E
authors: Mikiciuk-Olasik
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy / Q000503:physiopathology; D002091:Butyrylcholinesterase / Q000187:drug effects / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003124:Colorimetry; D000077265:Donepezil; D007189:Indans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D002800:Cholinesterase Inhibitors; D007189:Indans; D010880:Piperidines; C530514:hydrazinonictinamide; D009536:Niacinamide; D000077265:Donepezil; D002091:Butyrylcholinesterase