Xu Bing, Xu Xin, Zhang Chenze, Zhang Yuzhong, Wu GaoRong, Yan Mengmeng, Jia Menglu, Xie Tianxin, Jia Xiaohui, Wang Penglong, Lei Haimin
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
Department of Pathology, Beijing University of Chinese Medicine, Beijing, 100102 China.
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.
据报道，川芎嗪-香草酸衍生物具有良好的神经保护活性。在我们持续努力开发具有神经保护作用的新型川芎嗪衍生物的过程中，我们尝试合成了几种川芎嗪-香草酸酰胺衍生物，并筛选了它们对氯化钴损伤的PC12细胞的保护作用。结果表明，大多数新合成的衍生物表现出比川芎嗪更高的活性，其中化合物显示出最高的效力，其EC值为17.39±1.34μM。简要讨论了构效关系。
图形摘要
合成了一系列新的川芎嗪-香草酸酰胺衍生物，并评估了它们对氯化钴损伤的PC细胞的保护作用。发现是活性最高的一种。
