Synthesis and evaluation of anticonvulsant and antidepressant activities of 5-alkoxytetrazolo[1,5-c]thieno[2,3-e]pyrimidine derivatives

被引：51

作者：

Wang, Shi-Ben ^{[1
]}

Deng, Xian-Qing ^{[1
]}

Zheng, Yan ^{[1
]}

Yuan, Yan-Ping ^{[1
]}

Quan, Zhe-Shan ^{[1
]}

Guan, Li-Ping ^{[2
]}

机构：

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

[2] Zhejiang Ocean Univ, Food & Pharm Coll, Zhoushan 316004, Zhejiang, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 56卷

基金：

中国国家自然科学基金;

关键词：

Tetrazole; Anticonvulsant; Antidepressant; Forced swimming test; Open-field test; ANTIEPILEPTIC DRUG DEVELOPMENT; MICE; EPILEPSY; DEPRESSION; TETRAZOLE; MODELS; CYTOTOXICITY; DISORDERS;

D O I：

10.1016/j.ejmech.2012.08.027

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 5-alkoxytetrazolo[1,5-c]thieno[2,3-e]pyrimidine derivatives were synthesized and their anticonvulsant and antidepressant activities were evaluated. Pharmacological tests showed that four of the synthesized compounds had weak anticonvulsant activity, while most of the compounds had excellent antidepressant activity. The most active compound was 5-(2,4-dichlorobenzyloxy)tetrazolo [1,5-c] thieno[2,3-e]pyrimidine, which decreased the immobility time by 51.62% at a dose of 100 mg/kg. The results of open-field tests of this compound indicated that it had no significant effects on the locomotor activity compared with the control group at the doses assayed in the forced swimming tests test. This means that the antidepressant activity detected in the FST for the compound is not the result of central nervous system stimulant properties, and further confirms its antidepressant-like effect. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：139 / 144

页数：6

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