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为了寻找具有更好抗惊厥活性及低神经毒性的化合物,文章以6-羟基-3,4-二氢-2(1H)-喹啉酮为起始原料合成了4个2-取代-7-苄氧基-4,5-二氢-[1,2,4]三氮唑[4,3-a]喹啉-1(2H)-酮衍生物,对目标化合物,采用小鼠最大电惊厥实验(MES),皮下戊四唑实验(sc-PTZ)测定了其抗惊厥活性,采用旋转法测定了神经毒性。药理实验结果显示目标化合物表现出了较强的抗惊厥活性,该结论证明喹啉并三氮唑化合物具有被开发为新型癫痫治疗药的优良品质。
In order to search for compounds with better anticonvulsant activity and low neurotoxicity, four 2-substituted-7-chloro-4-hydroxy-3,4- Benzyloxy-4,5-dihydro- [1,2,4] triazolo [4,3-a] quinolin- 1 (2H) -one derivatives were tested for their maximum electroconvulsant The anticonvulsant activity was measured by MES and sc-PTZ, and the neurotoxicity was measured by spin method. Pharmacological results show that the target compound showed strong anticonvulsant activity. This conclusion proves that quinoline and triazole compounds have good qualities developed as novel epilepsy therapeutic drugs.