Abstract
Angular pyrrolocoumarins were synthesized from the reaction of 4-hydroxyindole or 5-hydroxyindole with DMAD and PPh(3) and were tested for anti-inflammatory and antioxidant activity. These compounds significantly inhibited the carrageenin-induced paw edema (60.5%-73.4%) and have important scavenging activity. Although their interaction with the free stable radical DPPH is not high, compound 9 is the most potent (73.4%) in the in vivo experiment. Compound 7 seems to be a potent LOX inhibitor. An attempt was made to correlate the biological results with their structural characteristics and physicochemical parameters.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Inflammatory Agents / chemical synthesis
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Anti-Inflammatory Agents / pharmacology
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Antioxidants / chemical synthesis
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Antioxidants / pharmacology
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Coumarins / chemical synthesis*
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Coumarins / pharmacology*
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Free Radical Scavengers / pharmacology
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Glycine max / enzymology
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Humans
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Lipoxygenase / metabolism
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Prothrombin Time
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Pyrroles / chemical synthesis*
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Pyrroles / pharmacology*
Substances
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Anti-Inflammatory Agents
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Antioxidants
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Coumarins
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Enzyme Inhibitors
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Free Radical Scavengers
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Pyrroles
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Lipoxygenase