4.7 Article

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

Journal

ACTA PHARMACEUTICA SINICA B
Volume 5, Issue 4, Pages 343-349

Publisher

INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
DOI: 10.1016/j.apsb.2015.01.008

Keywords

2,3-Dioxoindolin-1-acctamides; Synthesis; Anticonvulsant activity; Antidepressant activity; Pentylenetetrazole

Funding

  1. National Spark Plan Project of China [2013GA70025]
  2. Natural Science Foundation of Zhejiang Province of China [LY14C190001]

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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/).

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