Synthesis and Anti-ulcer Activities of Sodium Alkylazulene Sulfonates

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概要

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• Many derivatives of sodium alkylazulene sulfonates were newly synthesized and their antiulcer activites were examined in Shay pylorus-ligated rats. The values of lipophilicity (log P), a physicochemical parameter, of these new azulene derivatives were also examined in order to study the structure-activity relationship. The optimum value of log P which gave maximum anti-ulcer activity was about -1.0. Among the derivatives of azulene examined, 3-ethyl-7-isopropylazulene-1-sulfonic acid sodium salt (KT1-32) exhibited an extremely potent inhibitory action against Shay ulcer, and its antipeptic activity was more potent than than of guaiazulene sodium sulfonate (GAS). Furthermore, KT1-32 was extremely stable on heating as compared to GAS.

• 社団法人日本薬学会の論文
• 1988-02-25

著者

• 冨山 剛

  寿製薬株式会社 寿総合研究所

• 柳沢 隆

  Kotobuki Research Laboratories, Kotobuki Pharmaceutical Company, Ltd.,

• 冨山 剛

  Kotobuki Research Laboratories, Kotobuki Pharmaceutical Company, Ltd.,

• 柳沢 隆

  Kotobuki Research Laboratories Kotobuki Seiyaku Co. Ltd.

• 若林 修一

  Kotobuki Research Laboratories, Kotobuki Seiyaku Co., Ltd.,

• 安並 正文

  Department of Chemistry, Faculty of Science, Tohoku University

• 高瀬 嘉平

  Department of Chemistry, Faculty of Science, Tohoku University

• 安並 正文

  Department Of Chemistry Faculty Of Science Tohoku University

• 高瀬 嘉平

  Department Of Chemistry Faculty Of Science Tohoku University

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