Synthesis, anticonvulsant and neurotoxicity evaluation of some new pyrimidine-5-carbonitrile derivatives

被引：23

作者：

Shaquiquzzaman, Mohammad ^{[1
]}

Khan, Suroor Ahmad ^{[1
]}

Amir, Mohammad ^{[1
]}

Alam, Mohammad Mumtaz ^{[1
]}

机构：

[1] Jamia Hamdard, Fac Pharm, Dept Pharmaceut Chem, New Delhi 110062, India

来源：

SAUDI PHARMACEUTICAL JOURNAL | 2012年 / 20卷 / 02期

关键词：

Cyanopyrimidine; Schiff's base; Anticonvulsant activity; Neurotoxicity; Lipophilicity; PHARMACOLOGICAL EVALUATION; SEIZURE MODELS;

D O I：

10.1016/j.jsps.2011.09.007

中图分类号：

R9 [药学];

学科分类号：

1007 ;

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(-1) at 0.5 h time interval, indicating their ability to prevent seizure spread at a relatively low dose. (C) 2011 King Saud University. Production and hosting by Elsevier B. V. All rights reserved.

引用

页码：149 / 154

页数：6

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