Citation: Wen-Ya Wang, Cheng-Wu Shen, Zhi-Jie Weng, Tie-Chuang Wang, Chuang Zhang, Xun-Qi Jin, Jian-Qi Li. Design, synthesis and biological evaluation of novel dicarbonylalkyl piperazine derivatives as neuroprotective agents[J]. Chinese Chemical Letters, ;2016, 27(03): 387-390. doi: 10.1016/j.cclet.2015.11.002 shu

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

a.
a. Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai 201203, China;
b.
b. Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai 201203, China;
c.
c. Shandong Provincial Hospital Affiliated to Shandong University, Jinan 250021, China

Corresponding author: Jian-Qi Li,
Received Date: 14 July 2015
Available Online: 17 August 2015
Fund Project: This work was supported by Shanghai Natural Science Foundation (No.12ZR1450100). (No.12ZR1450100)

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.
- Dicarbonylalkyl piperazine,
- Neuroprotective,
- Ischemic stroke
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