synthesis and acetylcholinesterase inhibitory evaluation of 4-(1,3-dioxoisoindolin-2-yl)-n-phenylbenzamide derivatives as potential anti-alzheimer agents
نویسندگان
چکیده
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. phthalic anhydride was reacted with 4-aminobenzoic acid in the presence of triethylamine under reflux condtion. then, the obtained acidic derivative was utilized for preparation of final compounds via an amidation reaction through a carbodiimde coupling reaction. anti-acetylcholinesterase activity of synthesized derivatives was assessed by ellman's test. compound 4g in this series exhibited the highest inhibitory potency (ic50 = 1.1 ± 0.25 µm) compared to donepezil (ic50 = 0.41 ± 0.12 µm) as reference drug.
منابع مشابه
Synthesis 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 کاملSynthesis and Acetylcholinesterase Inhibitory Evaluation of 4-(1,3-Dioxoisoindolin-2-yl)-N-Phenyl Benzamide Derivatives as Potential Anti-Alzheimer Agents
Alzheimer᾽s disease is characterized by cognitive deficits, impaired long-term potentiation of 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 a...
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...
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عنوان ژورنال:
iranian journal of pharmaceutical researchجلد ۱۵، شماره ۳، صفحات ۳۱۳-۳۲۰
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