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
收藏
页码：409 / 414
页数：6
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