Synthesis and Anticonvulsant Activity of Some Cinnamylpiperazine Derivatives

被引:4
|
作者
Hu, Chuan [2 ]
Sun, Zhi-Gang [1 ]
Wei, Cheng-Xi [1 ,2 ]
Quan, Zhe-Shan [2 ]
机构
[1] Inner Mongolia Univ Nationalities, Inst Neurosurg, Tongliao City 028007, Inner Mongolia, Peoples R China
[2] Yanbian Univ, Coll Pharm, Yanji 133000, Jilin, Peoples R China
基金
中国国家自然科学基金;
关键词
Anticonvulsant; MES; Calcium channel; Flunarizine; Cinnarizine; Cinnamyl piperazine; FLUNARIZINE; EPILEPSY; MICE;
D O I
10.2174/157018010792929595
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of cinnamylpiperazine derivatives was synthesized using different benzophenone as starting material. The structures of the compounds were proved by their IR, H-1-NMR spectroscopic data and mass spectra data. The anticonvulsant activities of these compounds were evaluated with maximal electroshock (MES) test and rotarod test with intraperitoneal injection on KunMing mice. Among all the flunarizine analogues, no one exhibited better anticonvulsant activity than flunarizine. Flunarizine (4i) exhibited anticonvulsant activity with ED50 of 38.1 mg/kg, TD50 of 164.3 mg/kg and PI of 4.3 through administration intraperitoneal, and with ED50 of 56.8 mg/kg, TD50 of 456.3 mg/kg and PI of 8.0 through oral administration.
引用
收藏
页码:661 / 664
页数:4
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