2,3-DIHYDRO-1-BENZOFURAN-5-OLS AS ANALOGS OF ALPHA-TOCOPHEROL THAT INHIBIT IN-VITRO AND EX-VIVO LIPID AUTOXIDATION AND PROTECT MICE AGAINST CENTRAL-NERVOUS-SYSTEM TRAUMA

被引：41

作者：

GRISAR, JM ^{[1
]}

BOLKENIUS, FN ^{[1
]}

PETTY, MA ^{[1
]}

VERNE, J ^{[1
]}

机构：

[1] MARION MERRELL DOW RES INST,F-67080 STRASBOURG,FRANCE

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 38卷 / 03期

关键词：

D O I：

10.1021/jm00003a008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of a-tocopherol analogues was synthesized with potential therapeutic value for such pathological conditions as stroke and trauma. A set of criteria such as the inhibition of in vitro lipid peroxidation, superoxyl radical scavenging, and brain penetration, as measured by ex vivo inhibition of lipid peroxidation, was applied to select the most effective compound. 2,3-Dihydro-2,2,4,6,7-pentamethyl-3-[(4-methylpiperazino)methyl]-1-benzofuran-5-ol hydrochloride (22) was selected because of its superior antioxidant properties and better brain penetration. This compound also protected mice against the effects of head injury. The criteria thus turned out to be useful for the characterization of a neuroprotective analogue of alpha-tocopherol.

引用

页码：453 / 458

页数：6

共 24 条

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