摘要
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-α]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、^(13)C 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(ED_(50))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.
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^-1 and protective index (PI) value of 24.3, which was a potential anti-epilepsy candidate compound.
作者
李佳丽
胡涛
张洪健
宫国华
全哲山
Li Jiali;Hu Tao;Zhang Hongjian;Gong Guohua;Quan Zhe-Shan(College of Pharmacy,Yanbian University,Yanji 133002;Inner Mongolia Autonomous Region Key laboratory of Mongolian Medicine Pharmacology for Cardio-cerebral Vascular System,Tongliao 028000;Affiliated Hospital of Inner Mongolia University for Nationalities,Tongliao 028000)
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2018年第7期1673-1679,共7页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金(Nos.21662036
81660837)资助项目~~