Synthesis, anticonvulsant and neurotoxicity evaluation of some new pyrimidine-5-carbonitrile derivatives
- 作者：Mohammad Shaquiquzzaman ; shaqiq@gmail.com ; Suroor Ahmad Khan ; Mohammad Amir ; Mohammad Mumtaz Alam
- 关键词：Cyanopyrimidine ; Schiff&rsquo ; s base ; Anticonvulsant activity ; Neurotoxicity ; Lipophilicity
- 刊名：Journal of the Saudi Pharmaceutical Society
- 出版年：2012
- 期刊代码：P131_13190164
- 类别：pha
- 出版时间：April, 2012
- 卷：20
- 期：2
- 页码：149-154
- 文件大小：474 K
摘要
A series of 2-[2-(substituted benzylidene) hydrazinyl]-4-(4-methoxyphenyl)-6-oxo-1,6-dihydro-pyrimidine-5-carbonitrile (3-16) were synthesized by refluxing 2-hydrazino-4-(4-methoxy-phenyl)-6-oxo-1,6-dihydro-pyrimidine-5-carbonitrile (2) with different substituted aromatic aldehydes in glacial acetic acid and absolute alcohol mixture (8:2). The compounds were evaluated for their anticonvulsant and neurotoxicity effect. In MES test compounds 2-[2-(4-bromo-benzylidene)-hydrazinyl]-4-(4-methoxyphenyl)-6-oxo-1,6-dihydro-pyrimidine-5-carbonitrile (5), 2-[2-(4-hydroxy-benzylidene)-hydrazinyl]-4-(4-methoxyphenyl)-6-oxo-1,6-dihydro-pyrimidine-5-carbonitrile (9), and 2-[2-(3-fluoro-benzylidene)-hydrazinyl]-4-(4-methoxyphenyl)-6-oxo-1,6-dihydro-pyrimidine-5-carbonitrile (16) were found to be highly active at a dose level of 30 mgkg鈭? at 0.5 h time interval, indicating their ability to prevent seizure spread at a relatively low dose.