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Synthesis and Evaluation of Anti-acetylcholinesterase Activity of ۲-(۲-(۴-(۲-Oxo-۲-phenylethyl)piperazin-۱-yl) ethyl)Isoindoline-۱,۳-dione Derivatives with Potential Anti-Alzheimer Effects

محل انتشار: مجله علوم پایه پزشکی ایران، دوره: 16، شماره: 10
سال انتشار: 1392
نوع سند: مقاله ژورنالی
زبان: انگلیسی
مشاهده: 148

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https://civilica.com/doc/1298001

شناسه ملی سند علمی:

JR_IJBMS-16-10_003

تاریخ نمایه سازی: 4 آبان 1400

چکیده مقاله:

  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 acetylcholine (Ach) and therefore, through this mechanism improve the symptoms of AD. Materials and Methods: In the current study, based on the potential inhibitory activity of phthalimide derivatives towards acetylcholinesterase enzyme, a new series of phthalimide-based compounds were synthesized (۴a-۴e) and anti-acetylcholinesterase effect was assessed using Ellman's test. Compound ۴b with ۴-Fluorophenyl moiety was the most potent derivative in this series (IC۵۰ = ۱۶.۴۲ ± ۱.۰۷ μM). It was shown that, none of the synthesized compounds showed superior inhibitory potency compared to donepezil (۰.۴۱ ± ۰.۰۹ μM) as a reference drug.   Conclusion: The new synthesized phthalimide based analogs could function as potential acetylcholinesterase inhibitors. Further studies are necessary for development of potent analogs.

کلیدواژه ها:

Acetylcholinesterase Alzheimer Phthalimide Synthesis

نویسندگان

Alireza Aliabadi

۱Novel Drug Delivery Research Center, Kermanshah University of Medical Sciences, Kermanshah, Iran ۲Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran

Alireza Foroumadi

۳Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran

Ahmad Mohammadi-Farani

۱Novel Drug Delivery Research Center, Kermanshah University of Medical Sciences, Kermanshah, Iran.۴Department of Pharmacology, Toxicology and Medical Services, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran

Mahdi Garmsiri Mahvar

۲Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran۵Students Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran

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