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RESEARCH ARTICLE
Year : 2015  |  Volume : 4  |  Issue : 2  |  Page : 162-171

Synthesis and acetylcholinesterase inhibitory assessment of 3-(2-(4-benzoylpiperazin-1-yl) ethylimino) indolin-2-one derivatives with potential anti-alzheimer effects


1 Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences; Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
2 Department of Pharmacology, Toxicology and Medical Services, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
3 Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences; Students Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran
4 Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran

Correspondence Address:
Alireza Aliabadi
Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah
Iran
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Source of Support: None, Conflict of Interest: None


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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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