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Issue 3, 2017
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Design, synthesis and evaluation of new ligustrazine derivatives as potential plasma-stable neuroprotective agents

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Abstract

A series of ligustrazine–phenolic acid esters which exhibited promising neuroprotective activities have previously been reported. Nevertheless, we found that these ester compounds (like T-VA) were not stable in plasma by further in vivo studies. To investigate plasma-stable neuroprotective agents, a series of new ligustrazine derivatives were synthesized by conjoining ligustrazine and phenols with ester, ether and amide bonds. Most of the compounds exhibited higher protective effects against CoCl2-induced neurotoxicity in differentiated PC12 cells than ligustrazine. Structure–activity relationships were also briefly discussed. We found that compound 2c (2-((2-methoxy-4-(((3,5,6-trimethylpyrazin-2-yl)methoxy) methyl)phenoxy)methyl)-3,5,6-trimethylpyrazine) displayed the highest protective effect on the PC12 cells damaged by CoCl2 (EC50 = 1.07 μM). Preliminary stability investigation in rat plasma was verified in vitro and better plasma stability was observed with 2c in comparison to T-VA.

Graphical abstract: Design, synthesis and evaluation of new ligustrazine derivatives as potential plasma-stable neuroprotective agents

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Publication details

The article was received on 02 Jan 2017, accepted on 08 Feb 2017 and first published on 09 Feb 2017


Article type: Research Article
DOI: 10.1039/C7MD00003K
Citation: Med. Chem. Commun., 2017,8, 652-656
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    Design, synthesis and evaluation of new ligustrazine derivatives as potential plasma-stable neuroprotective agents

    C. Zhang, W. Yan, R. Zhao, B. Xu, X. Fang, M. Yan, Y. Zhang, P. Wang and H. Lei, Med. Chem. Commun., 2017, 8, 652
    DOI: 10.1039/C7MD00003K

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