Antiinflammatory activity of N-(2-benzoylphenyl)alanine derivatives

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 App...

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Veröffentlicht in:Journal of medicinal chemistry 1984-10, Vol.27 (10), p.1317-1321
Hauptverfasser: Walsh, David A, Sleevi, Mark C, Sancilio, Lawrence F
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00376a016