アンスラニル酸関連化合物の抗炎症作用(第1報) : N-フェニルアンスラニル酸誘導体について

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Twenty-nine N-phenylanthranilic acid derivatives were synthesized and their oral effectiveness on carrageenin-edema and cotton pellet-granuloma in rats, or UV-induced erythema in guinea pigs was tested. Intravenous acute toxicity of these compounds on mice was also examined. Anti-edema activity of N-phenylanthranilic acid (PA) was estimated to be almost equal to that of salicylic acid. N-(α-Naphthyl)anthranilic acid was more potent but showed higher acute toxicity than did PA or phenylbutazone. Methyl or chlorine substitution of PA enhanced both anti-inflammatory and toxic activities of the compounds, while carboxyl group, as well as amino or hydroxyl, considerably reduced these biological properties. Of the compounds tested, Flufenamic acid was the most active in all the three antiinflammatory assays. The derivatives related to Flufenamic acid were also active agents. However, no enhancement of toxicity was noted by trifluoromethyl substitution in PA and further no significant reduction of biological activities was observed by introduction of another carboxyl group to fulfenamic acid molecule, contrary to the case of methyl and chlorine substituted derivatives of PA. As an exception, it was found that four inactive compounds displayed relatively high toxicity on mice. In general, the biological activities did not varid with substituted position, but were markedly affected by the kind of substituent present.
公益社団法人日本薬学会の論文
1969-10-25

アンスラニル酸関連化合物の抗炎症作用(第1報) : N-フェニルアンスラニル酸誘導体について

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