School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, PR China.
School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, PR China.
Bioorg Chem. 2017 Aug;73:63-75. doi: 10.1016/j.bioorg.2017.05.010. Epub 2017 May 31.
Neuroprotection refers to the relative preservation of neuronal structure and function. Neuroprotective agents refer to substances that are capable of preserving brain function and structure. Currently, there are no neuroprotective agents available that can effectively relieve the progression of Parkinson's disease. In this work, five novel 4-aminopyridine derivatives, including three amides and two ureas, were designed, synthesized, and evaluated using the rat PC12 mice pheochromocytoma cell line as an in vitro model. As well as human Rho kinase inhibitory experiment was performed. Among them, compound 3, which exhibited high cell viability, low cytotoxicity and good efficacy of inhibition on α-synuclein, oxidation, inflammation and Rho kinase, was profound as potential agents for Parkinson's disease (PD).
神经保护是指神经元结构和功能的相对保留。神经保护剂是指能够保护脑功能和结构的物质。目前，尚无有效的神经保护剂可有效缓解帕金森病的进展。在这项工作中，设计、合成并评价了五个新型 4-氨基吡啶衍生物，包括三个酰胺和两个脲，采用大鼠 PC12 小鼠嗜铬细胞瘤细胞系作为体外模型。并进行了人 Rho 激酶抑制实验。其中，化合物 3 表现出高细胞活力、低细胞毒性和对α-突触核蛋白、氧化、炎症和 Rho 激酶的良好抑制作用，是帕金森病（PD）的潜在药物。
