Synthesis and Acetylcholinesterase Inhibitory Assessment of 3-(2-(4-benzoylpiperazin-1-yl) ethylimino) indolin-2-one Derivatives with Potential Anti-Alzheimer Effects

Marzieh Rahmani Khajouei; Ahmad Mohammadi-Farani; Hamid Ghorbani; Alireza Aliabadi

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Synthesis and Acetylcholinesterase Inhibitory Assessment of 3-(2-(4-benzoylpiperazin-1-yl) ethylimino) indolin-2-one Derivatives with Potential Anti-Alzheimer Effects

Author(s):

Marzieh Rahmani Khajouei^{1, 2},

Ahmad Mohammadi-Farani³,

Hamid Ghorbani^{2, 4},

Alireza Aliabadi^2,*

1Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran

2Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran

3Department of Pharmacology, Toxicology and Medical Services, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran

4Students Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran

Journal of Reports in Pharmaceutical Sciences:Vol. 4, issue 2; 162-171

Published online:Aug 31, 2015

Article type:Research Article

Received:Apr 14, 2015

Accepted:Jul 28, 2015

How to Cite:Marzieh Rahmani KhajoueiAhmad Mohammadi-FaraniHamid GhorbaniAlireza AliabadiSynthesis and Acetylcholinesterase Inhibitory Assessment of 3-(2-(4-benzoylpiperazin-1-yl) ethylimino) indolin-2-one Derivatives with Potential Anti-Alzheimer Effects.J Rep Pharm Sci.4(2):e147677.

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.

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