Paper Information

Journal:   IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES   OCTOBER 2013 , Volume 16 , Number 10; Page(s) 1049 To 1054.
 
Paper: 

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

 
 
Author(s):  ALIABADI ALIREZA*, FOROUMADI ALIREZA, MOHAMMADI FARANI AHMAD, GARMSIRI MAHVAR MAHDI
 
* NOVEL DRUG DELIVERY RESEARCH CENTER, KERMANSHAH UNIVERSITY OF MEDICAL SCIENCES, KERMANSHAH, IRAN
 
Abstract: 

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 (4a-4e) and anti-acetylcholinesterase effect was assessed using Ellman’s test. Compound 4b with 4-Fluorophenyl moiety was the most potent derivative in this series (IC50=16.42±1.07 mM). It was shown that, none of the synthesized compounds showed superior inhibitory potency compared to donepezil (0.41±0.09 mM) 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.

 
Keyword(s): ACETYLCHOLINESTERASE ALZHEIMER PHTHALIMIDE SYNTHESIS
 
References: 
  • ندارد
 
  pdf-File tarjomyar Yearly Visit 78
 
Latest on Blog
Enter SID Blog