Abstract
Tolfenamic acid esters with nitrooxyalcohols are synthesized. They are anti-inflammatory agents reducing carrageenan rat paw edema, with low gastrointestinal and general toxicity. In vitro, they are nitric oxide donors, inhibitors of lipoxygenase and cyclooxygenases. A two to three carbon chain between carboxylic and nitric ester groups seems optimal for activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents / adverse effects
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Anti-Inflammatory Agents / chemistry*
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Anti-Inflammatory Agents / pharmacology*
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Antioxidants / chemistry
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Antioxidants / pharmacology
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Cyclooxygenase 1 / metabolism
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Cyclooxygenase 2 / metabolism
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Female
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Hindlimb / drug effects
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Intestines / drug effects*
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Isoenzymes / metabolism
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Lipoxygenase / metabolism
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Male
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Molecular Structure
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Nitric Oxide / metabolism*
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Rats
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Stomach / drug effects*
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ortho-Aminobenzoates / adverse effects
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ortho-Aminobenzoates / chemistry*
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ortho-Aminobenzoates / pharmacology*
Substances
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Anti-Inflammatory Agents
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Antioxidants
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Enzyme Inhibitors
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Isoenzymes
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ortho-Aminobenzoates
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Nitric Oxide
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tolfenamic acid
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Lipoxygenase
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Cyclooxygenase 1
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Cyclooxygenase 2