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

Acta Pharmaceutica Sinica B

Xinghua Zhen¹  Yan Han¹  Zhou Peng¹  Shuilian Zhao¹  Liping Guan¹  Qinghao Jin² 

[1] Food and Pharmacy College, Zhejiang Ocean University and Zhejiang Provincial Engineering Technology Research Center of Marine Biomedical Products, Zhoushan 316022, China;Hailisheng Pharmaceutical Co., Lid., Zhoushan 316021, China;

关键词: 2,3-Dioxoindolin-1-acetamide;    Synthesis;    Anticonvulsant activity;    Antidepressant activity;    Pentylenetetrazole;   

DOI  :  10.1016/j.apsb.2015.01.008

来源: DOAJ

【 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.

【 授权许可】

Unknown