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

被引：0
作者：
Lamia Wagdy Mohamed
Mohamed F. El-yamany
机构：
[1] Cairo University,Organic Chemistry Department, Faculty of Pharmacy
[2] Cairo University,Pharmacology Department, Faculty of Pharmacy
[3] Cairo University,Organic Chemistry Department, Faculty of Pharmacy
来源：
Archives of Pharmacal Research | 2012年 / 35卷
关键词：
1,4-Benzodiazepine; Acetylcholine; Alzheimer’s disease; Cyclopenin; Cyclopenol;
D O I：
暂无
中图分类号：
学科分类号：
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.
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页码：1369 / 1377
页数：8
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