期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 3, 页码 1107-1112出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.12.006
关键词
Tropolone; Oxidative stress; Neuronal cell damage
资金
- Center for Drug Discovery, Northeastern University, Boston, USA
- EURODESY [MEST-CT2005-020575]
beta-Thujaplicin (hinokitiol or 2-hydroxy-4-isopropyl-2,4,6-cycloheptatrien-1-one), a natural tropolone, shows numerous activities while its synthetic analogues were found to exhibit anticancer and anti-ischemic activity. However, the ability of tropolone derivatives to protect neuronal cells from oxidative stress-induced cell damage has not been studied so far. As an ongoing effort toward highly effective antioxidants with potential neuroprotective activity, we have synthesized 7-substituted derivatives of beta-thujaplicin and its methoxy analogue. The substituents were heterocycles (piperazine, morpholine) or heteroaromatics (triazoles, pyridine). Only the piperazine derivatives of beta-thujaplicin were able to protect HT22 hippocampal neurons from oxidative stress-induced cell death. (C) 2010 Elsevier Masson SAS. All rights reserved.
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