Abstract
Compounds 4a-j and 5 were synthesized by cyclocondensation of 3a-j and hydrazine and showed significant LDL-antioxidant activities in the TBARS assay, the lag time of conjugated diene production, the relative electrophoretic mobility (REM) of ox-LDL, the apoB-100 fragmentation, and the macrophage-mediated LDL oxidation. Among compounds 4a-j and 5, 4a was found to be the most active compound as an inhibitor of LDL oxidation and 4a (IC50 = 0.1 microM) was 6-fold more potent than probucol (IC50 = 0.6 microM) in the TBARS assay.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antioxidants / chemical synthesis*
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Antioxidants / pharmacology
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Copper / pharmacology
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Humans
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Inhibitory Concentration 50
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Lipid Peroxidation / drug effects
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Lipoproteins, LDL / antagonists & inhibitors
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Lipoproteins, LDL / drug effects*
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Lipoproteins, LDL / metabolism
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Macrophages / metabolism
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Oxidation-Reduction
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Pyrazoles / chemical synthesis
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Pyrazoles / pharmacology*
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Thiobarbituric Acid Reactive Substances
Substances
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Antioxidants
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Lipoproteins, LDL
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Pyrazoles
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Thiobarbituric Acid Reactive Substances
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oxidized low density lipoprotein
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Copper