酞嗪并三唑或四唑類衍生物的合成及其抗驚厥活性研究
發(fā)布時間:2019-01-04 18:04
【摘要】:設(shè)計合成了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]酞嗪四個系列16個衍生物.其化學(xué)結(jié)構(gòu)均經(jīng)過1H NMR、13C NMR、IR和HRMS確征.藥理方面,利用最大電驚厥法(MES),以小鼠腹腔給藥測定其抗驚厥活性.實驗結(jié)果顯示N-(4-溴苯基)-四唑[5,1-a]酞嗪-6-胺(7a)的抗驚厥活性最強,其半數(shù)有效量ED50為5.89 mg·kg-1,抗驚厥作用強于對照藥卡馬西平.
[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.
【作者單位】: 延邊大學(xué)藥學(xué)院;
【基金】:國家自然科學(xué)基金(No.21272005)資助項目~~
【分類號】:O626;TQ460.1
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本文編號: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.
【作者單位】: 延邊大學(xué)藥學(xué)院;
【基金】:國家自然科學(xué)基金(No.21272005)資助項目~~
【分類號】:O626;TQ460.1
,
本文編號:2400612
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