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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.
Li, Shulin; Wei, Daiyan; Mao, Zhuo; Chen, Ligong; Yan, Xilong; Li, Yang; Dong, Shengjie; Wang, Donghua.
Afiliação
  • Li S; School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, PR China.
  • Wei D; School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, PR China.
  • Mao Z; School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, PR China.
  • Chen L; School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, PR China.
  • Yan X; School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, PR China.
  • Li Y; School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, PR China.
  • Dong S; School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, PR China.
  • Wang D; School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, PR China. Electronic address: dhwang022@163.com.
Bioorg Chem ; 73: 63-75, 2017 08.
Article em En | MEDLINE | ID: mdl-28618343
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).
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Doença de Parkinson / Desenho de Fármacos / 4-Aminopiridina / Fármacos Neuroprotetores / Inibidores de Proteínas Quinases / Simulação de Acoplamento Molecular Idioma: En Ano de publicação: 2017 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Doença de Parkinson / Desenho de Fármacos / 4-Aminopiridina / Fármacos Neuroprotetores / Inibidores de Proteínas Quinases / Simulação de Acoplamento Molecular Idioma: En Ano de publicação: 2017 Tipo de documento: Article