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Design, synthesis, immunocytochemistry evaluation, and molecular docking investigation of several 4-aminopyridine derivatives as potential neuroprotective agents for treating Parkinson’s disease.

Authors :
Li, Shulin
Wei, Daiyan
Mao, Zhuo
Chen, Ligong
Yan, Xilong
Li, Yang
Dong, Shengjie
Wang, Donghua
Source :
Bioorganic Chemistry. Aug2017, Vol. 73, p63-75. 13p.
Publication Year :
2017

Abstract

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). [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
00452068
Volume :
73
Database :
Academic Search Index
Journal :
Bioorganic Chemistry
Publication Type :
Academic Journal
Accession number :
124187348
Full Text :
https://doi.org/10.1016/j.bioorg.2017.05.010