- 著者
- 鶴田 峯生 三ケ島 浩 大江 孝範 川崎 和幸 瀬戸口 信郎 中 洋一 田原 哲治
- 出版者
- 公益社団法人 日本薬学会
- 雑誌
- YAKUGAKU ZASSHI (ISSN:00316903)
- 巻号頁・発行日
- vol.109, no.1, pp.33-45, 1989-01-25 (Released:2008-05-30)
- 参考文献数
- 28
- 被引用文献数
- 7 5
Several imidazolylpyridinemethanols and imidazolylbenzenemethanols were prepared and evaluated for an inhibitory activity against arachidonic acid-induced platelet aggregation. The result shows that the arylmethanol moiety is essential for the activity and may correspond to the 15-OH group of prostagrandin H2 (PGH2). Among the compounds tested, 4-[α-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3, 5-dimethylbenzoic acid (XV) was found to have a potent inhibitory activity and a long duration of action. Structureactivity relationships are also discussed briefly.
- 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
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.