Antiinflammatory agents. 1. Synthesis and antiinflammatory activity of 2-amino-3-benzoylphenylacetic acid

The synthesis and antiinflammatory activity of 2-amino-3-benzoylphenylacetic acid are described. This compound was postulated to be an active metabolite of 7-benzoylindoline in order to explain the unexpected antiinflammatory activity of the latter compound. Metabolism studies on 14C-labeled 7-benzo...

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Veröffentlicht in:	Journal of medicinal chemistry 1979-09, Vol.22 (9), p.1074-1079
Hauptverfasser:	Welstead, William J, Moran, H. Wayne, Stauffer, Harold F, Turnbull, Lennox B, Sancilio, Lawrence F
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Inflammatory Agents - chemical synthesis Arthritis, Experimental - drug therapy Benzophenones - chemical synthesis Benzophenones - metabolism Benzophenones - pharmacology Benzophenones - therapeutic use Biotransformation Female In Vitro Techniques Male Phenylacetates - chemical synthesis Phenylacetates - metabolism Phenylacetates - pharmacology Phenylacetates - therapeutic use Pleural Effusion - drug therapy Rats
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Zusammenfassung:	The synthesis and antiinflammatory activity of 2-amino-3-benzoylphenylacetic acid are described. This compound was postulated to be an active metabolite of 7-benzoylindoline in order to explain the unexpected antiinflammatory activity of the latter compound. Metabolism studies on 14C-labeled 7-benzoylindoline did not confirm this hypothesis. Nevertheless, 2-amino-3-benzoylphenylacetic acid, its ethyl ester, and the sodium salt show potent antiinflammatory activity in pharmacological models.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00195a012