850415-38-2Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel dicarbonylalkyl piperazine derivatives as neuroprotective agents
Wang, Wen-Ya,Shen, Cheng-Wu,Weng, Zhi-Jie,Wang, Tie-Chuang,Zhang, Chuang,Jin, Xun-Qi,Li, Jian-Qi
supporting information, p. 387 - 390 (2016/03/16)
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.
The design and synthesis of 1,4-substituted piperazine derivatives as triple reuptake inhibitors
Han, Minsoo,Han, Younghue,Song, Chiman,Hahn, Hoh-Gyu
, p. 2597 - 2602 (2012/10/29)
Novel 1,4-substituted piperazine derivatives 5, Series A and B were designed by fragment analysis and molecular modification of 4 selected piperazine-containing compounds which possess antidepressant activity. We synthesized new 39 analogues of Series A and 10 compounds of Series B, respectively. The antidepressant screening against DA, NE, and serotonin neurotransmitter uptake inhibition was carried out using the Neurotransmitter Transporter Uptake Assay Kit. The compounds in Series B showed relatively higher reuptake inhibitory activity for SERT, NET, and DAT than those in Series A. The length of spacer between the central piperazine core and the terminal phenyl ring substituted at the piperazine ring in Series B seems to exert an important role in the activity.
