Synthesis and Evaluation of Some New (1,2,4) Triazolo(4,3-a)Quinoxalin-4(5H)-one Derivatives as AMPA Receptor Antagonists

被引:36
作者
Abul-Khair, Hamada [1 ]
Elmeligie, Salwa [2 ]
Bayoumi, Ashraf [1 ]
Ghiaty, Adel [1 ]
El-Morsy, Ahmed [1 ]
Hassan, Memy H. [3 ]
机构
[1] Al Azhar Univ, Dept Organ Chem, Fac Pharm, Cairo 11884, Egypt
[2] October 6 Univ, Dept Organ Chem, Fac Pharm, Sixth Of October City 12585, Egypt
[3] Al Azhar Univ, Dept Pharmacol & Toxicol, Fac Pharm, Cairo 11884, Egypt
关键词
ANTIEPILEPTIC DRUGS;
D O I
10.1002/jhet.714
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
This study involves the synthesis and anticonvulsant evaluation of 1-ethyl-3-hydrazinylquinoxaline-2-(1H)-one (8), its chemical confirmations 9 and 10 and certain (1,2,4) triazolo(4,3-a)quinoxalin-4(5H)-one compounds 11, 12, 13, 13a, 13b, 13c, 13d, 13e, 13f, 14, 15, 16. The structure of the synthesized compounds was confirmed chemically by elemental analyses and spectral data (IR, 1H NMR, 13C NMR, and Mass). Docking studies were preformed to all of the synthesized compounds to predict, in a qualitative way, the anticonvulsant activity of the proposed compounds. There is a promising correlation between the results of molecular modeling and the anticonvulsant activity of the synthesized compounds. The highest fitting value was noticed for compounds 9 and 10, which showed the highest anticonvulsant activity.
引用
收藏
页码:1202 / 1208
页数:7
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