Synthesis and Anticonvulsant Activity Evaluation of Some 1-alkoxy-4-(1H-1,2,4-triazol-1-yl)phthalazines

被引：6

作者：

Wang, Shi-Ben ^{[1
]}

Deng, Xian-Qing ^{[1
]}

Song, Ming-Xia ^{[1
]}

Quan, Zhe-Shan ^{[1
]}

机构：

[1] Yanbian Univ, Coll Pharm, Yanji 133002, Jilin, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2012年 / 9卷 / 04期

基金：

中国国家自然科学基金;

关键词：

Anticonvulsant; 2,3-Dihydrophthalazine-1,4-dione; 1H-1,2,4-Triazole; Phthalazine; Maximal Electroshock; Neurotoxicity; ANTIEPILEPTIC DRUG DEVELOPMENT; DERIVATIVES; DESIGN; INHIBITORS;

D O I：

10.2174/157018012799860024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1-alkoxy-4-(1H-1,2,4-triazol-1-yl)phthalazine derivatives were synthesized using 2,3-dihydrophthalazine-1,4-dione as starting material. The structures of the compounds were characterized by elemental analysis, IR, H-1-NMR and MS data. Anticonvulsant activities of these compounds were evaluated by maximal electroshock (MES) test following intraperitoneal injection in mice. Among the synthesized compounds 3a-3t, compound 3e was the most active compound with an ED50 of 28.9 mg/kg, TD50 of 173.6 mg/kg and protective index (PI) of 6.0.

引用

页码：409 / 414

页数：6

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