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

作     者：Wen-Ya Wang Cheng-Wu Shen Zhi-Jie Weng Tie-Chuang Wang Chuang Zhang Xun-Qi Jin Jian-Qi Li 

作者机构：Novel Technology Center of Pharmaceutical Chemistry Shanghai Institute of Pharmaceutical Industry Shanghai 201203 China Shanghai Engineering Research Center of Pharmaceutical Process Shanghai 201203 China Shandong Provincial Hospital Affiliated to Shandong University Jinan 250021 China 

基　　金：supported by Shanghai Natural Science Foundation(No.12ZR1450100) 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2016年第27卷第3期

页      码：387-390页

摘      要：In the search of novel neuroprotective agents with higher potency than our previously identified antiischemic 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.

主 题 词：Dicarbonylalkyl piperazine Neuroprotective Ischemic stroke 

学科分类：1007[医学-药学类] 081704[081704] 07[理学] 08[工学] 0817[工学-轻工类] 070303[070303] 0703[理学-化学类] 100701[100701] 10[医学] 

核心收录：

D　O　I：10.1016/j.cclet.2015.11.002

馆 藏 号：203846273...