Design and synthesis of novel 1,4-benzodiazepine derivatives and their biological evaluation as cholinesterase inhibitors

被引：11
|
作者：
Mohamed, Lamia W. [1 ]
El-yamany, Mohamed F. [2 ]
机构：
[1] Cairo Univ, Fac Pharm, Dept Organ Chem, Cairo 11562, Egypt
[2] Cairo Univ, Fac Pharm, Dept Pharmacol, Cairo 11562, Egypt
来源：
ARCHIVES OF PHARMACAL RESEARCH | 2012年 / 35卷 / 08期
关键词：
1,4-Benzodiazepine; Acetylcholine; Alzheimer's disease; Cyclopenin; Cyclopenol; CYCLOPENIN;
D O I：
10.1007/s12272-012-0806-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new series of 1,4-benzodiazepine-2,5-dione structurally related to cyclopenin has been synthesized. The new compounds were assayed in vivo and in vitro for their ability to inhibit acetylcholinesterase enzyme and were found to have potent reversible anticholinesterase activity when tested in vitro for isolated frog rectus abdominis and guinea pig ileum in addition to increasing brain cholinesterase level in rats when percentage inhibition were tested in vivo, moreover compounds 5a, 5b, 5c and 5g were the most active. LD50 was performed for these derivatives and they displayed high safety margin.
引用
收藏
页码：1369 / 1377
页数：9
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