Abstract
A series of lipoamino acids were synthesized and their neuroprotective effect against brain ischemia induced by oxygen-glucose deprivation (OGD) on rat cerebral slices was evaluated. Among these compounds, N-stearoyl-L-tyrosine (4), N-stearoyl-L-serine (5) and N-stearoyl-L-threonine (6) exhibited good neuroprotective activity. We found that the neuroprotective activity of lipoamino acids depended on the acyl group, the presence of a free carboxylic function and a free hydroxyl group at the branched chain of the amino acids. The results also showed that 5 was the most active compound, protecting rat brain slices against OGD as well as hydrogen peroxide (H(2)O(2)) insult at the range of 1-10 M.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anaerobiosis
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Animals
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Brain / blood supply
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Brain / drug effects*
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Brain Ischemia / prevention & control*
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Hydrogen Peroxide / toxicity
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Neuroprotective Agents / chemical synthesis
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Neuroprotective Agents / chemistry
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Neuroprotective Agents / pharmacology*
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Rats
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Serine / analogs & derivatives*
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Serine / chemical synthesis
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Serine / chemistry
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Serine / pharmacology
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Threonine / analogs & derivatives*
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Threonine / chemical synthesis
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Threonine / chemistry
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Threonine / pharmacology
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Tyrosine / analogs & derivatives*
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Tyrosine / chemical synthesis
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Tyrosine / chemistry
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Tyrosine / pharmacology
Substances
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N-stearoyl-L-serine
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N-stearoyl-L-threonine
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Neuroprotective Agents
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Threonine
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Tyrosine
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Serine
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N-stearoyltyrosine
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Hydrogen Peroxide