Synthesis and Studies of 4-Phenylthiazol-2(3H)-one Derivatives as New Anticonvulsant Agents

被引：0

作者：

Deng, Xian-Qing ^{[1
]}

Song, Ming-Xia ^{[1
]}

Liu, Bing ^{[1
]}

Xiao, Lin ^{[1
]}

Zou, Jia-Xing ^{[1
]}

Li, Tuan ^{[1
]}

Chen, Wen-Xing ^{[1
]}

Chen, Li-Zhi ^{[1
]}

机构：

[1] Jinggangshan Univ, Coll Med, Jian 343009, Jiangxi, Peoples R China

来源：

LATIN AMERICAN JOURNAL OF PHARMACY | 2014年 / 33卷 / 09期

关键词：

Anticonvulsant; Maximal electroshock; Neurotoxicity; Pentylenetetrazole; Thiazolone; ANTIEPILEPTIC DRUG DEVELOPMENT; THIAZOLIDINONE DERIVATIVES; PHENYTOIN DERIVATIVES; EPILEPSY; DESIGN; GABA;

D O I：

暂无

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The present study described the syntheses and anticonvulsant activity evaluation of 4-(substituted-phenyl)thiazol-2(3H)-one derivatives (3a-3m). The results demonstrated that most compounds exhibited potent anticonvulsant activity in the maximal electroshock test. Among which, 4-(4-pentyloxyphenyl) thiazol-2(3H)-one (3k) emerged as the most promising candidate on the basis of its favorable ED50 value of 12.2 mg/ kg and protective index (PI) value of 20.8. The high PI value offered it a wider safety margin than the clinic drugs carbamazepine, phenobarbital, and valproate. In addition, the potence of compound 3k against seizures induced by pentylenetetrazole suggested that 3k maybe exert anticonvulsant activity through affecting GABAergic system.

引用

页码：1430 / 1435

页数：6

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