Synthesis and protective effect of new ligustrazine-vanillic acid derivatives against CoCl(2)-induced neurotoxicity in differentiated PC12 cells

Ligustrazine-vanillic acid derivatives had been reported to exhibit promising neuroprotective activities. In our continuous effort to develop new ligustrazine derivatives with neuroprotective effects, we attempted the synthesis of several ligustrazine-vanillic acid amide derivatives and screened the...

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Detalles Bibliográficos
Autores principales: Xu, Bing, Xu, Xin, Zhang, Chenze, Zhang, Yuzhong, Wu, GaoRong, Yan, Mengmeng, Jia, Menglu, Xie, Tianxin, Jia, Xiaohui, Wang, Penglong, Lei, Haimin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer International Publishing 2017
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5331027/
https://www.ncbi.nlm.nih.gov/pubmed/28293281
http://dx.doi.org/10.1186/s13065-017-0250-z
Descripción
Sumario:Ligustrazine-vanillic acid derivatives had been reported to exhibit promising neuroprotective activities. In our continuous effort to develop new ligustrazine derivatives with neuroprotective effects, we attempted the synthesis of several ligustrazine-vanillic acid amide derivatives and screened their protective effect on the injured PC12 cells damaged by CoCl(2). The results showed that most of the newly synthesized derivatives exhibited higher activity than ligustrazine, of which, compound VA-06 displayed the highest potency with EC(50) values of 17.39 ± 1.34 μM. Structure-activity relationships were briefly discussed. [Figure: see text]

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