Inhibitory Effect of 2-(E-2-Alkenoylamino)ethyl Alkyl sulfides on Gastric Ulceration in Rats. II. Structure and Activity Relationships of 2-(E-n or Z-n-Decenoylamino)ethyl Alkyl Sulfides

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概要

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• The analogues of 2-(E-n or Z-n-decenoylamino)ethyl carbamoylmethyl sulfide, including the modifications of sulfide portion, double bond in decenoyl chain and alkyl sulfide moiety, were synthesized and their inhibitory effects on stress-induced ulceration in rats were compared.Replacing the sulfura atom by methylene group or oxygen atom reduced the effect of potency. Saturation of the double bond in the decenoyl chain tended to reduce the anti-ulcerogenic activity in rats. There was no relationship between the position of double bond in decenoyl chain and the pharmacological activity. On the other hand, compounds with E-configuration showed stronger anti-ulcer activity than the corresponding Z-type of compounds. Among 9 kinds of S substituted alkyl groups for carbamoylmethyl, 2-(E-2-decenoylamino)ethyl 2-cyclohexylethyl sulfide showed the most potent anti-ulcerogenic activity in rats and also showed the lowest acute toxicity in mice.

• 公益社団法人日本薬学会の論文
• 1991-06-25

著者

• 横山 和正

  Central Research Laboratory, Green Cross Corporation

• 小浜 靖弘

  Faculty of Pharmaceutical Sciences, Osaka University

• 小濱 靖弘

  大阪大学 薬 微薬品化

• 三村 務

  Faculty of Pharmaceutical Sciences, Osaka University

• 横山 和正

  株式会社ミドリ十字中央研究所

• 甲田 伊佐男

  Central Reserach Laboratories, The Green Cross Corporation

• 岩井 正和

  Central Reserach Laboratories, The Green Cross Corporation

• 渡辺 正弘

  Central Reserach Laboratories, The Green Cross Corporation

• KOHDA Isao

  Japan and Central Research Laboratories, Green Cross Corporation, Ltd.,

• 三村 務

  大阪大学薬学部

• 小浜 靖弘

  大阪大学薬学部

• 甲田 伊佐男

  Central Research Laboratories The Green Cross Corporation

• 岩井 正和

  Central Research Laboratories The Green Cross Corporation

• 深谷 力

  Research Division The Green Cross Corporation

• 深谷 力

  Central Research Laboratories, Green Cross Corporation

• 荒川 良夫

  Central Research Laboratories, The Green Cross Corporation

• 荒川 良夫

  Central Research Laboratories The Green Cross Corporation

• 横山 和正

  株式会社ミドリ十字 中央研究所

• 横山 和正

  Central Research Laboratories The Green Cross Corporation

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