title: Synthesis and protective effect of new ligustrazine-vanillic acid derivatives against CoCl2-induced neurotoxicity in differentiated PC12 cells.
abstract: 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 CoCl2. The results showed that most of the newly synthesized derivatives exhibited higher activity than ligustrazine, of which, compoundVA-06displayed the highest potency with EC50values 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 PC12cells damaged by CoCl2.VA-06was found to be the most active one.
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: Bing
authors.initials: B
authors.lastname: Xu
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: Xin
authors.initials: X
authors.lastname: Xu
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: Chenze
authors.initials: C
authors.lastname: Zhang
authors.affiliation: Department of Pathology, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: Yuzhong
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: GaoRong
authors.initials: G
authors.lastname: Wu
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: Mengmeng
authors.initials: M
authors.lastname: Yan
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: Menglu
authors.initials: M
authors.lastname: Jia
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: Tianxin
authors.initials: T
authors.lastname: Xie
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Jia
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: Penglong
authors.initials: P
authors.lastname: Wang
authors.affiliation: School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, 100102 China.
authors.forename: Haimin
authors.initials: H
authors.lastname: Lei
keywords: Neuroprotective effect; PC12 cell; Synthesis; T-VA amide derivatives