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设计合成了6-取代-1,2,4-三氮唑并[3,4-a]酞嗪和6-取代四氮唑并[5,1-a]酞嗪四个系列16个衍生物.其化学结构均经过1H NMR、13C NMR、IR和HRMS确征.药理方面,利用最大电惊厥法(MES),以小鼠腹腔给药测定其抗惊厥活性.实验结果显示N-(4-溴苯基)-四唑[5,1-a]酞嗪-6-胺(7a)的抗惊厥活性最强,其半数有效量ED50为5.89 mg·kg-1,抗惊厥作用强于对照药卡马西平.
A series of 16 derivatives of 6-substituted-1,2,4-triazolo [3,4-a] phthalazine and 6-substituted tetrazolino [5,1-a] phthalazine were designed and synthesized Its chemical structure was confirmed by 1H NMR, 13C NMR, IR and HRMS.Pharmacological aspects, the use of maximum electroconvulsive method (MES), its anti-convulsive activity was measured intraperitoneally in mice.The experimental results show N- (4- Bromophenyl) -tetrazol [5,1-a] phthalazin-6-amine (7a) showed the strongest anticonvulsant activity with an ED50 of 5.89 mg · kg-1 and a strong anticonvulsant effect Carbamazepine.