Synthesis and biological evaluation of some novel quinoxaline derivatives as anticonvulsant agents

被引:0
|
作者
Elhelby, Abdelghany Aly [2 ]
Ayyad, Rezk Rezk [2 ]
Zayed, Mohamed Fathalla [1 ,2 ]
机构
[1] Taibah Univ, Dept Pharmaceut Chem, Fac Pharm Boys, Al Madinah Al Munawarah, Saudi Arabia
[2] Al Azhar Univ, Dept Pharmaceut Chem, Fac Pharm Boys, Cairo, Egypt
来源
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH | 2011年 / 61卷 / 07期
关键词
Anticonvulsant drugs; Arylidene; Quinoxaline derivatives; Synthesis; ANTAGONISTS;
D O I
暂无
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 new derivatives of quinonxaline (V1 - 7) were designed and synthesized by condensation of different aromatic aldehydes with 2-(2-oxo-3-phenylquinoxalin-1(2H)-yl)acetohydrazide (IV). All synthesized compounds were isolated and confirmed by IR, H-1-NMR, MS, elemental analysis and then tested as anticonvulsant agents. Compound V-3 and V-1 showed the highest anticonvulsant effect with anticonvulsant potency relative to phenobarbital sodium of 0.8 and 0.75 whereas compound V-5 exhibited the lowest relative potency of 0.09. The other compounds showed variable activity between these values as follows: V-2 = 0.19, V-4 = 0.41, V-6 = 0.1 and V-7 = 0.15. All compounds showed less activity than the reference compound phenobarbital. But the compounds provided a basis for further optimization.
引用
收藏
页码:379 / 381
页数:3
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