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

被引：31

作者：

Zayed, Mohamed F. ^{[1
,4
]}

Ahmed, Hany E. A. ^{[1
,5
]}

Omar, Abdel-Sattar M. ^{[2
,4
]}

Abdelrahim, Adel S. ^{[3
,4
]}

El-Adl, Khaled ^{[4
]}

机构：

[1] Taibah Univ, Coll Pharm, Dept Pharmaceut Chem, Al Madinah Al Munawarah, Saudi Arabia

[2] King Abdulaziz Univ, Fac Pharm, Dept Pharmaceut Chem, Jeddah 21413, Saudi Arabia

[3] Jazan Univ, Dept Pharmaceut Chem, Fac Pharm, Jazan, Saudi Arabia

[4] Al Azhar Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, Egypt

[5] Al Azhar Univ, Fac Pharm, Dept Organ Chem, Cairo, Egypt

来源：

MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 12期

关键词：

Quinazolin-4(3H)-one; Epilepsy; Neurotoxicity; Synthesis; Anticonvulsant;

D O I：

10.1007/s00044-013-0569-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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.

引用

页码：5823 / 5831

页数：9

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