摘要/Abstract

设计合成了一系列6-取代-吡啶并[3，2-e][1，2，4]三唑并[4，3-a]吡嗪类衍生物，分别采用最大电惊厥法（MES）和旋转棒法测定其对小鼠的抗惊厥活性及神经毒性.其化学结构均经过¹H NMR、¹³C NMR、MS和HRMS进行确征.实验结果显示，6-苯氧基-吡啶并[3，2-e][1，2，4]三唑并[4，3-a]吡嗪（5g）的半数有效剂量（ED₅₀）为93.9 mg·kg^-1，保护指数为24.3，其安全性高于对照药卡马西平，是一种潜在的抗癫痫候选化合物.
关键词: 酞吡啶并[2,3-b]吡嗪, 三唑, 合成, 抗惊厥, 最大电惊厥法
In this paper, a series of 6-substituted-pyrido[3,2-e] [1,2,4]triazolo[4,3-a]pyrazine derivatives have been synthesized. Their anticonvulsant activity and neurotoxicity in mice were evaluated by maximal electroshock (MES) and rotarod test, respectively. The structures were confirmed by ¹H NMR, ¹³C NMR, MS and HRMS. The experimental results show that 6-phenoxypyrido[3,2-e] [1,2,4]triazolo[4,3-a]pyrazine (5g) was safer than the reference drug, carbamazepine, with ED₅₀value of 93.9 mg·kg^-1and protective index (PI) value of 24.3, which was a potential anti-epilepsy candidate compound.
Key words: pyrido[2,3-b]pyrazine, triazole, synthesis, anticonvulsant, the maximal electroshock


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