Design, synthesis, and biological evaluation studies of novel quinazolinone derivatives as anticonvulsant agents

被引:0
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作者
Mohamed F. Zayed
Hany E. A. Ahmed
Abdel-Sattar M. Omar
Adel S. Abdelrahim
Khaled El-Adl
机构
[1] College of Pharmacy,Pharmaceutical Chemistry Department
[2] Taibah University,Pharmaceutical Chemistry Department, Faculty of Pharmacy
[3] King AbdulAziz University,Pharmaceutical Chemistry Department, Faculty of Pharmacy
[4] Jazan University,Pharmaceutical Chemistry Department, Faculty of Pharmacy
[5] Al-Azhar University,Organic Chemistry Department, Faculty of Pharmacy
[6] Al-Azhar University,undefined
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关键词
Quinazolin-4(3H)-one; Epilepsy; Neurotoxicity; Synthesis; Anticonvulsant;
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摘要
In view of their expected anticonvulsant activity, some novel derivatives of 6,8-diiodo-2-methyl-3-substituted-quinazolin-4(3H)-ones (4–14) were synthesized, evaluated for their anticonvulsant activity by the maximal electroshock-induced seizure and subcutaneous pentylenetetrazole tests. The neurotoxicity was assessed using rotorod test. All the tested compounds showed considerable anticonvulsant activity in at least one of the anticonvulsant tests. Compounds 5, 6, and 8 proved to be the most potent compounds of this series with relatively low neurotoxicity and low toxicity in the median lethal dose test when compared with the reference drugs. The obtained results showed that the most potent compounds could be useful as a template for future design, optimization, and investigation to produce more active analogs.
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页码:5823 / 5831
页数:8
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