Synthesis and anticonvulsant activity evaluation of 8-alkoxy-5-(4H-1,2,4-triazol-4-yl)quinoline derivatives

被引:0
作者
Shi-Ben Wang
Xian-Qing Deng
Yan Zheng
Hong-Jian Zhang
Zhe-Shan Quan
机构
[1] Yanbian University,College of Pharmacy
[2] Jinggangshan University,Medical College
来源
Archives of Pharmacal Research | 2013年 / 36卷
关键词
Synthesis; Anticonvulsant; Quinoline; Triazole; Triazolone; Maximal electroshock;
D O I
暂无
中图分类号
学科分类号
摘要
Two series of 8-alkoxy-5-(4H-1,2,4-triazol-4-yl)quinolines and 8-alkoxy-5-(2H-1,2,4-triazol-3-one-4-yl)quinolines were synthesized. The anticonvulsant activity of these compounds was evaluated with maximal electroshock seizure test and rotarod test. Among the synthesized compounds, 8-octoxy-5-(4H-1,2,4-triazol-4-yl)quinoline (4g) was the most active compound with ED50 of 8.80 mg/kg, TD50 of 176.03 mg/kg and protective index of 20.0. Its neurotoxicity was lower than all other synthesized compounds and also markedly lower than that of the reference drug carbamazepine. In addition, the potency of compound 4g against seizures induced by pentylenetetrazole, 3-mercaptopropionic acid, and bicuculline suggested its broad spectrum activity, and the mechanisms of action including inhibition of voltage-gated ion channels and modulation of GABAergic activity might involve in its anticonvulsant activity.
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页码:32 / 40
页数:8
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