Abstract
Six novel ibuprofen derivatives and related structures, incorporating a proline moiety and designed for neurodegenerative disorders, are studied. They possess anti-inflammatory properties and three of them inhibited lipoxygenase. One compound was found to inhibit cyclooxygenase (COX)-2 production in spleenocytes from arthritic rats. The HS-containing compounds are potent antioxidants and one of them protected against glutathione loss after cerebral ischemia/reperfusion. They demonstrated lipid-lowering ability and seem to acquire low gastrointestinal toxicity. Acetylcholinesterase inhibitory activity, found in two of these compounds, may be an asset to their actions.
MeSH terms
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Animals
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Antioxidants / chemical synthesis
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Antioxidants / pharmacology
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Arthritis, Experimental / drug therapy
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Arthritis, Experimental / enzymology
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Biphenyl Compounds
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Blood-Brain Barrier / metabolism
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Cholesterol / blood
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Cholinesterase Inhibitors / chemical synthesis
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Cholinesterase Inhibitors / pharmacology
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Cyclooxygenase 2 Inhibitors / chemical synthesis
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Cyclooxygenase 2 Inhibitors / pharmacology
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Freund's Adjuvant
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Gastrointestinal Diseases / chemically induced
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Gastrointestinal Diseases / pathology
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Glutathione / metabolism
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Hyperlipidemias / blood
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Hypoxia-Ischemia, Brain / drug therapy
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Ibuprofen / analogs & derivatives*
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Ibuprofen / chemical synthesis*
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Ibuprofen / pharmacology
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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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Mice
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Microsomes, Liver / drug effects
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Microsomes, Liver / metabolism
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Neuroprotective Agents / chemical synthesis*
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Neuroprotective Agents / pharmacology*
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Neuroprotective Agents / toxicity
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Nootropic Agents / chemical synthesis*
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Nootropic Agents / pharmacology*
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Nootropic Agents / toxicity
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Oxidative Stress / drug effects
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Picrates / antagonists & inhibitors
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Picrates / toxicity
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Rats
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Spleen / cytology
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Spleen / enzymology
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Triglycerides / blood
Substances
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Antioxidants
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Biphenyl Compounds
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Cholinesterase Inhibitors
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Cyclooxygenase 2 Inhibitors
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Lipoxygenase Inhibitors
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Neuroprotective Agents
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Nootropic Agents
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Picrates
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Triglycerides
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Freund's Adjuvant
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Cholesterol
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1,1-diphenyl-2-picrylhydrazyl
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Glutathione
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Ibuprofen