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

被引:19
作者
Zhen, Xinghua [1 ,2 ]
Peng, Zhou [1 ,2 ]
Zhao, Shuilian [1 ,2 ]
Han, Yan [1 ,2 ]
Jin, Qinghao [3 ]
Guan, Liping [1 ,2 ]
机构
[1] Zhejiang Ocean Univ, Food & Pharm Coll, Zhoushan 316022, Peoples R China
[2] Zhejiang Prov Engn Technol Res Ctr Marine Biomed, Zhoushan 316022, Peoples R China
[3] Hailisheng Pharmaceut Co Ltd, Zhoushan 316021, Peoples R China
关键词
2,3-Dioxoindolin-1-acctamides; Synthesis; Anticonvulsant activity; Antidepressant activity; Pentylenetetrazole; ANTIEPILEPTIC DRUG DEVELOPMENT; BEHAVIORAL DESPAIR; MANNICH-BASES; MICE; DESIGN; TESTS;
D O I
10.1016/j.apsb.2015.01.008
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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/).
引用
收藏
页码:343 / 349
页数:7
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