Abstract
A series of N-(2-benzoylphenyl)alanine derivatives were synthesized and tested for antiinflammatory activity in the Evans blue-carrageenan induced pleural effusion assay. The target compounds were envisioned to bind to a receptor site on the cyclooxygenase enzyme by a mechanism first proposed by Appleton and Brown. Of the 21 compounds prepared, two were found to be one-tenth as potent as indomethacin in the pleurisy model and one compound was tested and found to be weakly active in the adjuvant arthritis model.
MeSH terms
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Animals
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Anti-Inflammatory Agents / chemical synthesis*
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Arthritis / drug therapy*
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Arthritis, Experimental / drug therapy*
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Chemical Phenomena
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Chemistry
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Disease Models, Animal
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Indicators and Reagents
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Indomethacin / therapeutic use
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Phenylalanine / analogs & derivatives*
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Phenylalanine / chemical synthesis
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Phenylalanine / therapeutic use
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Pleurisy / drug therapy
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Rats
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents
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Indicators and Reagents
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Phenylalanine
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N-(2-benzoylphenyl)alanine
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Indomethacin