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KMID : 0043320120350081369
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Archives of Pharmacal Research
2012 Volume.35 No. 8 p.1369 ~ p.1377
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Design and synthesis of novel 1,4-benzodiazepine derivatives and their biological evaluation as cholinesterase inhibitors
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Mohamed Lamia Wagdy
El yamany Mohamed F.
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Abstract
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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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KEYWORD
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1,4-Benzodiazepine, Acetylcholine, Alzheimer’s disease, Cyclopenin, Cyclopenol
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