Yajun Bai, Xirui He, Yujun Bai, Ying Sun, Zefeng Zhao, Xufei Chen, Bin Li, Jing Xie, Yang Li, Pu Jia, Xue Meng, Ye Zhao, Yanrui Ding, Chaoni Xiao, Shixiang Wang, Jie Yu, Sha Liao, Yajun Zhang, Zhiling Zhu, Qiang Zhang, Yuhui Zhao, Fanggang Qin, Yi Zhang, Xiaoyang Wei, Min Zeng, Jing Liang, Ye Cuan, Guangzhi Shan, Tai-Ping Fan, Biao Wu, Xiaohui Zheng
Inspired by the traditional Chinese herbal pair of Polygala tenuifolia-Acori Tatarinowii for treating epilepsy, 33 novel substituted cinnamic α-asaronol esters and analogues were designed by Combination of Traditional Chinese Medicine Molecular Chemistry (CTCMMC) strategy, synthesized and tested systematically not only for anticonvulsant activity in three mouse models but also for LDH inhibitory activity. Thereinto, 68-70 and 75 displayed excellent and broad spectra of anticonvulsant activities with modest ability in preventing neuropathic pain, as well as low neurotoxicity...
December 1, 2019: European Journal of Medicinal Chemistry