神经保护
疾病
依达拉奉
冲程(发动机)
氧化应激
缺血
药理学
痴呆
化学
阿尔茨海默病
神经科学
医学
内科学
心理学
生物化学
机械工程
工程类
作者
Ruolin Cao,Fangyu Du,Yu Cui,M. Qi,Jun Zhuang,Jieru Wang,Maoying Zhang,Xiaoyu Zhang,Zhongbo Liu,Libo Zou,Wei Xiao,Guoliang Chen
标识
DOI:10.1016/j.bioorg.2023.107064
摘要
Alzheimer's disease, the commonest cause of dementia, is a growing global health concern with huge implications for individuals and society. Stroke has still been a significant challenge in clinics for a long time, which is the second leading cause of death in the world, especially ischemic stroke. Both Alzheimer's disease and stroke are closely related to oxidative stress and HIF-1 signaling pathways in nerve cells. Herein, we describe our structure-based design, synthesis, and biological evaluation of a new class of 8-biaryl-2,2-dimethylbenzopyranamide derivatives as natural product derivatives. Our efforts have resulted in the discovery of highly potent neuroprotective agents, as exemplified by compound D13 as a HIF-1α inhibitor, which significant improvement in the behavior of Alzheimer's disease mice and shows great potential improvement of brain infarct volume in pMCAO model rats, improves the increase of blood-brain barrier permeability after cerebral ischemia in rats, neuroprotective effect, reduce the level of apoptotic cells in rats after cerebral ischemia, better than Edaravone.
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