ahr-5850 and Pleural-Effusion

Several substituted 2-aminophenylacetic acid derivatives were prepared and tested for in vitro prostaglandin synthetase inhibition activity and for in vivo antiinflammatory activity. The 2-amino substituent is beneficial to potency in the inhibition of prostaglandin synthetase for the 3-phenoxy, 4-phenyl, and 3-benzoyl series, but only the 3-benzoyl series shows increased antiinflammatory potency in the in vivo assay.

Topics: Animals; Anti-Inflammatory Agents; Carrageenan; Cattle; Chemical Phenomena; Chemistry; Cyclooxygenase Inhibitors; In Vitro Techniques; Male; Molecular Conformation; Phenylacetates; Pleural Effusion

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.

Topics: Animals; Anti-Inflammatory Agents; Arthritis, Experimental; Benzophenones; Biotransformation; Female; In Vitro Techniques; Male; Phenylacetates; Pleural Effusion; Rats