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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Maher, Pamela
Kraus, Jean-Louis
description 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.
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subjects Amines - chemistry
Amines - pharmacology
Animals
Antioxidants
Biological and medical sciences
Cell death
Cell Death - drug effects
Cell Line
Hippocampus - cytology
Medical sciences
Mice
N, N-Bis-(8-hydroxyquinoline-5-yl methyl)-benzyl substituted amines
Neurons - drug effects
Neuropharmacology
Neuroprotection
Neuroprotective agent
Neuroprotective Agents - chemistry
Neuroprotective Agents - pharmacology
Oxidative Stress - drug effects
Oxyquinoline - chemistry
Oxyquinoline - pharmacology
Pharmacology. Drug treatments
PPAR gamma - agonists
PPAR-γ agonists
title N, N-Bis-(8-hydroxyquinoline-5-yl methyl)-benzyl substituted amines (HQNBA): Peroxisome proliferator-activated receptor (PPAR-γ) agonists with neuroprotective properties
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