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一些含1,2,4-三唑结构的新型酰腙化合物的合成及其在Neuro-2a细胞中的促神经突生长活性

Synthesis of some new acylhydrazone compounds containing the 1,2,4-triazole structure and their neuritogenic activities in Neuro-2a cells.

作者信息

Jiang Xia, Tang Genyun, Yang Jie, Ding Jiacheng, Lin Hongwei, Xiang Xiaoliang

机构信息

Key Laboratory of Research and Utilization of Ethnomedicinal Plant Resources of Hunan Province, College of Biological and Food Engineering, Huaihua University Huaihua 418008 P. R. China

Hunan Engineering Laboratory for Preparation Technology of Polyvinyl Alcohol (PVA) Fiber Material, College of Chemistry and Materials Engineering, Huaihua University Huaihua 418008 P. R. China

出版信息

RSC Adv. 2020 May 19;10(32):18927-18935. doi: 10.1039/d0ra02880k. eCollection 2020 May 14.

Abstract

In the present study, a novel series of acylhydrazone compounds (A0-A10) with the structure of 1,2,4-triazole have been designed and synthesized. In addition, all the synthesized compounds have been evaluated for neuritogenic activity in mouse neuroblastoma (Neuro-2a) cells. Notably, we found that one of these 11 acylhydrazone compounds, compound A5 (2-(4-amino-5-(pyridin-4-yl)-4-1,2,4-triazol-3-ylthio)-'-(2-hydroxybenzylidene)-acetohydrazide) displays excellent neuritogenic activity. Moreover, our present study revealed that compound A5 had the ability to induce neurite outgrowth through the PI3K/Akt and MEK-ERK signaling pathway in Neuro-2a cells. These findings suggest that compound A5 might exert neuritogenic effects and thus may be useful for the treatment of neural repair and regeneration.

摘要

在本研究中,设计并合成了一系列具有1,2,4-三唑结构的新型酰腙化合物(A0 - A10)。此外,对所有合成的化合物在小鼠神经母细胞瘤(Neuro-2a)细胞中的促神经突生长活性进行了评估。值得注意的是,我们发现这11种酰腙化合物中的一种,化合物A5(2-(4-氨基-5-(吡啶-4-基)-4-1,2,4-三唑-3-基硫代)-N'-(2-羟基亚苄基)-乙酰肼)表现出优异的促神经突生长活性。此外,我们目前的研究表明,化合物A5能够通过PI3K/Akt和MEK-ERK信号通路在Neuro-2a细胞中诱导神经突生长。这些发现表明,化合物A5可能发挥促神经突生长作用,因此可能对神经修复和再生治疗有用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c646/9053900/5163279f371d/d0ra02880k-s1.jpg

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