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
DOI:10.1016/j.cclet.2015.11.002
日期:2016.3
Abstract 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
摘要为了寻找比我们先前确定的抗缺血性中风候选药物1更高效力的新型神经保护剂,合成了一系列新型二羰基哌嗪衍生物,并通过氧-葡萄糖剥夺试验在类神经元PC12中评估了它们的神经保护活性。细胞,小鼠耐缺氧模型和大鼠局灶性脑缺血模型。获得的结果表明化合物7f,7k和7o表现出神经保护活性。特别地,含有2,5-二甲基哌嗪部分的化合物7o显示出小鼠的寿命延长和大鼠的脑梗塞减少,这为神经保护剂的开发提供了潜在的候选者。