Synthesis, potential anticonvulsant and antidepressant effects of 2-(5-methyl-2,3-dioxoindolin-1-yl)acetamide derivatives

• 作者: Liping Guan Qinghao Jin Shuilian Zhao Xinghua Zhen Yan Han Zhou Peng
• 来源期刊: 药学学报:英文版
• 学科: 医学
• 关键词: 2,3-Dioxoindolin-1-acctamides Synthesis Anticonvulsant activity Antidepressant activity Pentylenetetrazole
• 年，卷（期）: 2015,（4）
• 页码范围: 343-349
• 页数: 7页
• 分类号: R914.5
• 语种: 中文

摘要

A new series of 2-(5-methyl-2,3-dioxoindolin-1-yl)acetamide derivatives were synthesized and evaluated for their anticonvulsive activity in a pentylenetetrazole(PTZ)-evoked convulsion model and antidepressant activity in the forced swimming test(FST) model. Eleven synthesized compounds were found to be protective against PTZ-induced seizure and showed the anticonvulsant activity. In addition,four of the synthesized compounds(4l, 4m, 4p and 4q) showed potent antidepressant-like activity.Among these compounds, compound 4l was found to have the most potent antidepressant-like activity,and significantly reduced the duration of immobility time at 100 mg/kg dose level when compared to the vehicle control, which is similar to the reference drug fluoxetine.