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

نویسندگان

marzieh rahmani-khajouei

ahmad mohammadi-farani

hamid ghorbani

alireza aliabadi

چکیده

a b s t r a c t   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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synthesis and evaluation of anti-acetylcholinesterase activity of 2-(2-(4-(2-oxo-2-phenylethyl)piperazin-1-yl) ethyl)isoindoline-1,3-dione derivatives with potential anti-alzheimer effects

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عنوان ژورنال:
journal of reports in pharmaceutical sciences

جلد ۴، شماره ۲، صفحات ۱۴۸-۱۵۷

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