Synthesis and Acetylcholinesterase Inhibitory Evaluation of 4-(1,3-Dioxoisoindolin-2-yl)-N-Phenyl Benzamide Derivatives as Potential Anti-Alzheimer Agents

被引:0
|
作者
Mohammadi-Farani, Ahmad [1 ,2 ]
Darbandi, Samira Soltani [3 ,4 ]
Aliabadi, Alireza [1 ,4 ]
机构
[1] Kermanshah Univ Med Sci, Fac Pharm, Pharmaceut Sci Res Ctr, Kermanshah, Iran
[2] Kermanshah Univ Med Sci, Toxicol & Med Serv, Fac Pharm, Dept Pharmacol, Kermanshah, Iran
[3] Kermanshah Univ Med Sci, Students Res Comm, Kermanshah, Iran
[4] Kermanshah Univ Med Sci, Fac Pharm, Dept Med Chem, Kermanshah, Iran
来源
IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH | 2016年 / 15卷 / 03期
关键词
Synthesis; Phthalimide; Acetylcholinesterase; Alzheimer; ANTICHOLINESTERASE ACTIVITY; DESIGN; DISEASE; DOCKING; SERIES;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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. Phthalic anhydride was reacted with 4-aminobenzoic acid in the presence of triethylamine under reflux condition. 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 mu M) compared to donepezil (IC50 = 0.41 +/- 0.12 mu M) as reference drug.
引用
收藏
页码:313 / 320
页数:8
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