新型川芎嗪-香草酸衍生物的合成及其对CoCl诱导的分化型PC12细胞神经毒性的保护作用

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

作者信息

Xu Bing, Xu Xin, Zhang Chenze, Zhang Yuzhong, Wu GaoRong, Yan Mengmeng, Jia Menglu, Xie Tianxin, Jia Xiaohui, Wang Penglong, Lei Haimin

机构信息

School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.

Department of Pathology, Beijing University of Chinese Medicine, Beijing, 100102 China.

出版信息

Chem Cent J. 2017 Feb 28;11:20. doi: 10.1186/s13065-017-0250-z. eCollection 2017.

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. The results showed that most of the newly synthesized derivatives exhibited higher activity than ligustrazine, of which, compound displayed the highest potency with EC values of 17.39 ± 1.34 μM. Structure-activity relationships were briefly discussed.Graphical abstractNew series of ligustrazine-vanillic acid amide derivatives were synthesized and evaluated for their protective effect on the injured PC cells damaged by CoCl. was found to be the most active one.