Design, synthesis and biological evaluation of novel dicarbonylalkyl piperazine derivatives as neuroprotective agents

作者

Wang, WY;Shen, CW;Weng, ZJ;Wang, TC;Zhang, C;Jin, XQ;Li, JQ

作者单位

[Wang, Wen-Ya; Weng, Zhi-Jie; Wang, Tie-Chuang; Zhang, Chuang; Jin, Xun-Qi; Li, Jian-Qi] Shanghai Inst Pharmaceut Ind, Novel Technol Ctr Pharmaceut Chem, Shanghai 201203, Peoples R China.;-;[Wang, Wen-Ya; Weng, Zhi-Jie; Wang, Tie-Chuang; Zhang, Chuang; Jin, Xun-Qi; Li, Jian-Qi] Shanghai Engn Res Ctr Pharmaceut Proc, Shanghai 201203, Peoples R China.;-;[Shen, Cheng-Wu] Shandong Univ, Shandong Prov Hosp, Jinan 250021, Peoples R China.

摘要

In the search of novel neuroprotective agents with higher potency than our previously identified anti-ischemic stroke drug candidate 1, a series of novel dicarbonyl piperazine derivatives were synthesized and evaluated on their neuroprotective activity via oxygen-glucose deprivation test in the neuron-like PC12 cells, hypoxia tolerance model in mice and focal cerebral ischemia model in rats. The result obtained indicated that compounds 7f, 7k and 7o, exhibited neuroprotective activity. Particularly, compound 7o containing 2,5-dimethylpiperazin moiety, showed prolonged life time of mice and reduced cerebral infarction of rats, which provided a potential candidate for the development of neuroprotective agents. (C) 2015 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

关键词

ACUTE ISCHEMIC-STROKE; INJURY; DL-3-N-BUTYLPHTHALIDE; EDARAVONE; PENUMBRA; UPDATE

基本信息

所属机构:

归属医师: 沈承武

UT：000374799400018

刊名:CHINESE CHEMICAL LETTERS

年，卷(期):2016年27卷3期

页码：387-390

DOI：10.1016/j.cclet.2015.11.002

附件：

收录: SCIE