化学
特罗洛克
MPTP公司
神经保护
帕金森病
苯胺
抗氧化剂
药理学
多巴胺
螯合作用
铅化合物
化学合成
体外
组合化学
生物化学
疾病
抗氧化能力
有机化学
医学
内科学
作者
Zhongcheng Cao,Xianwu Fu,Xingyue Wang,Tianlong Zhang,Lei Zhong,Qian Xia,Jiang Zhu
标识
DOI:10.1016/j.ejmech.2023.115142
摘要
To discover novel multifunctional agents for the treatment of Parkinson's disease, a series of 2-hydroxyl-4-benzyloxybenzyl aniline derivatives was designed, synthesized and evaluated. The biological screening indicated that representative compound 6h possessed excellent MAO-B inhibition (IC50 = 0.014 μM), high antioxidant activity (ORAC = 2.14 Trolox equivalent), good metal chelating ability, appropriate BBB permeability and significant neuroprotective effect. Additionally, 6h exhibited great ability to alleviate the neuroinflammtion by suppressing the activation of NF-κB pathway in vitro. Furthermore, 6h can also ameliorate MPTP induced Parkinson's disease symptoms in mice by improving the dopamine level and repressing oxidative damage. These results indicated that compound 6h was a promising candidate for further development against PD.
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