Novel dual inhibitors of calpain and lipid peroxidation

被引:20
作者
Auvin, S
Pignol, B
Navet, E
Pons, D
Marin, JG
Bigg, D
Chabrier, PE
机构
[1] Inst Henri Beaufour, Ipsen Res Labs, Dept Med Chem, F-91966 Les Ulis, France
[2] Inst Henri Beaufour, Ipsen Res Labs, Dept Neurobiol, F-91966 Les Ulis, France
关键词
calpain inhibition; antioxidants;
D O I
10.1016/j.bmcl.2004.04.105
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of molecules with dual inhibitory activities on calpain and lipid peroxidation were synthesized. These hybrid compounds were built on the calpain pharmacophore 2-hydroxytetrahydrofuran linked to a set of antioxidants via a L-leucine linker. Compound 7, the most potent in cellular calpain and lipid peroxidation inhibitions, provided effective protection against glial cell death induced by maitotoxin. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3825 / 3828
页数:4
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