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

Synthesis, potential anticonvulsant and antidepressant effects of 2-(5-methyl-2,3-dioxoindolin-1-yl)acetamide derivatives
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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. A new series of 2-(5-methyL2,3-dioxoindolin-1 y)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 he protective against PTZ-induced seizure and showed the anticonvulsant activity. In addition, four of the synthesized compounds (41, 4m, 4p and 4q) showed potent antidepressant-like activity. Among these compounds, compound 41 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 lluoxetine. (C) 2015 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical. Sciences. Production and hosting by Elsevier BAT. This is an open access article under the CC BY-NC-ND licenses (http://creativecommons.org/licenses/by-nc-nd/4.0/).
出处 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2015年第4期343-349,共7页 药学学报(英文版)
基金 supported by the National Spark Plan Project of China (No. 2013GA70025) the Natural Science Foundation of Zhejiang Province of China (No. LY14C190001)
关键词 2 3-Dioxoindolin-1acetamide SYNTHESIS Anticonvulsant activity Antidepressant activity Pentylenetetrazole 2,3-Dioxoindolin-1-acctamides Synthesis Anticonvulsant activity Antidepressant activity Pentylenetetrazole
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  • 2李清华,植物学报,1987年,29卷,67页
  • 3岳旺,药学学报,1984年,19卷,16页
  • 4岳旺,中国药理学报,1984年,5卷,79页

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