synthesis and acetylcholinesterase inhibitory assessment of 3-(2-(4-benzoylpiperazin-1-yl) ethylimino)indolin-2-one derivatives with potential anti-alzheimer effects
نویسندگان
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.
منابع مشابه
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
Objective(s): Alzheimer's disease (AD) is a neurodegenerative disorder in elderly patients. Decrease in cholinergic neurotransmission is the main known cause in the pathophysiology of the disease. Improvement and potentiation of the cholinergic system could be beneficial for treatment of the AD. Acetylcholinesterase inhibitors such as donepezil can enhance the duration of action of a...
متن کاملSynthesis and acetylcholinesterase inhibitory evaluation of 4-(1,3-Dioxoisoindolin-2-yl)-N-phenylbenzamide derivatives as potential anti-alzheimer agents
Patients with Alzheimer's disease have cognitive deficits, impaired long-term potentiation and learning and memory. A progressive reduction in cholinergic neurons in some areas of the brain such as cortex and hippocampus is related to the deficits in memory and cognitive function in Alzheimer’s disease (AD). In the current project a new series of phthalimide derivatives were synthesized. Phthal...
متن کاملSynthesis and acetylcholinesterase inhibitory evaluation of 4-(1,3-Dioxoisoindolin-2-yl)-N-phenylbenzamide derivatives as potential anti-alzheimer agents
Patients with Alzheimer's disease have cognitive deficits, impaired long-term potentiation and learning and memory. A progressive reduction in cholinergic neurons in some areas of the brain such as cortex and hippocampus is related to the deficits in memory and cognitive function in Alzheimer’s disease (AD). In the current project a new series of phthalimide derivatives were synthesized. Phthal...
متن کامل2-(2-(4-Benzoylpiperazin-1-yl)ethyl)isoindoline-1,3-dione derivatives: Synthesis, docking and acetylcholinesterase inhibitory evaluation as anti-alzheimer agents
Objective(s): Alzheimer’s disease (AD) as progressive cognitive decline and the most common form of dementia is due to degeneration of the cholinergic neurons in the brain. Therefore, administration of the acetylcholinesterase (AChE) inhibitors such as donepezil is the first choice for treatment of the AD. In the present study, we focused on the synthesis and anti-cholinesterase evaluation of n...
متن کاملsynthesis 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
objective(s): alzheimer's disease (ad) is a neurodegenerative disorder in elderly patients. decrease in cholinergic neurotransmission is the main known cause in the pathophysiology of the disease. improvement and potentiation of the cholinergic system could be beneficial for treatment of the ad. acetylcholinesterase inhibitors such as donepezil can enhance the duration of action of acetylc...
متن کاملsynthesis and acetylcholinesterase inhibitory evaluation of 4-(1,3-dioxoisoindolin-2-yl)-n-phenylbenzamide derivatives as potential anti-alzheimer agents
patients with alzheimer's disease have cognitive deficits, impaired long-term potentiation and learning and memory. a progressive reduction in cholinergic neurons in some areas of the brain such as cortex and hippocampus is related to the deficits in memory and cognitive function in alzheimer’s disease (ad). in the current project a new series of phthalimide derivatives were synthesized. p...
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عنوان ژورنال:
journal of reports in pharmaceutical sciencesجلد ۴، شماره ۲، صفحات ۱۴۸-۱۵۷
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