N, N-Bis-(8-hydroxyquinoline-5-yl methyl)-benzyl substituted amines (HQNBA): Peroxisome proliferator-activated receptor (PPAR-γ) agonists with neuroprotective properties

N, N-Bis-(8-hydroxyquinoline-5-yl methyl)-benzyl substituted amines (HQNBA) are new peroxisome proliferator-activated receptor (PPAR-γ) agonists, which exert neuroprotective effects on lesionned HT22 cells. We report on the neuroprotective effects of N, N-bis-(8-hydroxyquinoline-5-yl methyl)-benzyl...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (23), p.6966-6968
Hauptverfasser: Madonna, Sébastien, Maher, Pamela, Kraus, Jean-Louis
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Sprache:eng
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Zusammenfassung:N, N-Bis-(8-hydroxyquinoline-5-yl methyl)-benzyl substituted amines (HQNBA) are new peroxisome proliferator-activated receptor (PPAR-γ) agonists, which exert neuroprotective effects on lesionned HT22 cells. We report on the neuroprotective effects of N, N-bis-(8-hydroxyquinoline-5-yl methyl)-benzyl substituted amines (HQNBA) in a model of oxidative stress-induced nerve cell death using mouse hippocampal-derived HT22 cells. The four derivatives (JLK1472, JLK1486, JLK1522 and JLK1535) protected the HT22 cells from death at concentrations ranging from 0.1 to 1 μM. Their action is partially dependent on their ability to act as PPARγ agonists. These analogues also maintain GSH levels suggesting that they have indirect anti-oxidant effects.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.09.134