著者

川崎 和幸 山田 一磨呂 大江 孝範 鶴田 峯生 寺澤 道夫 今吉 朋憲 安永 幸弘 後藤 一洋

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.109, no.11, pp.827-834, 1989-11-25

被引用文献数

3

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The pro-drugs of α, 2-dimethyl-5H-[1] benzopyrano [2,3-b] pyridine-7-acetic acid (I) with a potent anti-inflammatory activity were synthesized in order to reduce its gastrointestinal side effects. Various esters synthesized were evaluated for their anti-inflammatory activity and ulcerogenicity. Among the compounds maintaining a potent activity of I, N, N-dimethylcarbamoyl-methyl α, 2-dimethyl-5H-[1] benzopyrano [2,3-b] pyridine-7-acetate (II-18) showed excellent biopharmaceutical characteristics. The ulcerogenic effect of II-18 showed excellent biopharmaceutical characteristics. The ulcerogenic effect of II-18 on the rat gastric mucosa was about 3 times less than that of I. It was suggested that II-18 may be an useful biolabile pro-drug for I among the compounds tested.