Abstract
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.
MeSH terms
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Antioxidants / chemical synthesis*
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Antioxidants / pharmacology
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Calpain / antagonists & inhibitors*
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Calpain / metabolism
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Cell Death / drug effects*
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Furans / chemistry
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Humans
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Inhibitory Concentration 50
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Leucine / chemistry
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Lipid Peroxidation / drug effects*
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Lipoxygenase Inhibitors / chemical synthesis*
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Lipoxygenase Inhibitors / pharmacology
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Neuroglia
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Structure-Activity Relationship
Substances
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Antioxidants
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Furans
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Lipoxygenase Inhibitors
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Calpain
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Leucine