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Synthesis of tropolone derivatives and evaluation of their in vitro neuroprotective activity.

Abstract：

: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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Koufaki M,Theodorou E,Alexi X,Nikoloudaki F,Alexis MN

doi

10.1016/j.ejmech.2009.12.006

subject

Has Abstract

pub_date

2010-03-01 00:00:00

pages

1107-12

issue

3

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(09)00632-1

journal_volume

45

pub_type

杂志文章

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