酞嗪并三唑或四唑类衍生物的合成及其抗惊厥活性研究
发布时间:2019-01-04 18:04
【摘要】: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.
[Abstract]:Four series of 16 derivatives of 6-substituted-1-triazo-4-triazolazo [34-a] phthalazine and 6- substituted tetrazolazo [5anila-a] phthalazine were designed and synthesized. Their chemical structures were confirmed by 1H NMR,13C NMR,IR and HRMS. In pharmacology, the maximal electric convulsion method (MES),) was used to determine the anticonvulsant activity of mice intraperitoneally. The results showed that N- (4- bromophenyl) -tetrazole [51-a] phthalazine-6-amine (7a) had the strongest anticonvulsant activity, and its half effective dose (ED50) of 5.89 mg kg-1, was stronger than that of carbamazepine.
【作者单位】: 延边大学药学院;
【基金】:国家自然科学基金(No.21272005)资助项目~~
【分类号】:O626;TQ460.1
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本文编号:2400612
[Abstract]:Four series of 16 derivatives of 6-substituted-1-triazo-4-triazolazo [34-a] phthalazine and 6- substituted tetrazolazo [5anila-a] phthalazine were designed and synthesized. Their chemical structures were confirmed by 1H NMR,13C NMR,IR and HRMS. In pharmacology, the maximal electric convulsion method (MES),) was used to determine the anticonvulsant activity of mice intraperitoneally. The results showed that N- (4- bromophenyl) -tetrazole [51-a] phthalazine-6-amine (7a) had the strongest anticonvulsant activity, and its half effective dose (ED50) of 5.89 mg kg-1, was stronger than that of carbamazepine.
【作者单位】: 延边大学药学院;
【基金】:国家自然科学基金(No.21272005)资助项目~~
【分类号】:O626;TQ460.1
,
本文编号:2400612
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