Title of article :
Synthesis and Acetylcholinesterase Inhibitory Assessment of 3-(2-(4-benzoylpiperazin-1-yl) ethylimino) indolin-2-one Derivatives with Potential Anti-Alzheimer Effects
Author/Authors :
Rahmani-Khajouei, Marzieh Pharmaceutical Sciences Research Center - School of Pharmacy - Kermanshah University of Medical Sciences, Kermanshah , Mohammadi- Farani, Ahmad Department of Pharmacology - Toxicology and Medical Services - Faculty of Pharmacy - Kermanshah University of Medical Sciences , Ghorbani, Hamid Department of Medicinal Chemistry - Faculty of Pharmacy - Kermanshah University of Medical Sciences , Aliabadi, Alireza Department of Medicinal Chemistry - Faculty of Pharmacy - Kermanshah University of Medical Sciences
Abstract :
Alzheimer's disease (AD) is a neurodegenerative disorder in geriatric people
that characterized by reduction in memory and learning ability. Attenuation of
cholinergic system is the most likely hypothesis. Therefore, potentiation of the
cholinergic system via inhibition of acetylcholinesterase enzyme could
improve and alleviate the symptoms of AD. A new series of isatin-based
derivatives (4a-4h) were designed and synthesized according to the
pharmacophore of donepezil and consequently related anti-cholinesterase
effect was evaluated by Ellman's test. Obtained results were compared with
donepezil as a standard drug. All of target derivatives (4a-4h) synthesized
with moderate yields. In Ellman's test as an enzymatic assay for
acetylcholinesterase, the most of them displayed better inhibitory potency in
comparison with donepezil. In summary, isatin-based derivatives could be
potential anti-Alzheimer agents. But, more experimental investigations are
needed to prove this statement in the future.
Keywords :
Acetylcholinesterase , Anti-Alzheimer , Isatin , Synthesis
Journal title :
Astroparticle Physics