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...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.展开更多
基金supported by the National Spark Plan Project of China (No. 2013GA70025)the Natural Science Foundation of Zhejiang Province of China (No. LY14C190001)
文摘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.