Inhibitory Effect of 2-(E-2-Alkenoylamino)ethyl Alkyl Sulfides on Gastric Ulceration in Rats. I. Effect of 2-(E-2-Alkenoylamino)ethyl Carbamoylmethyl Sulfides on Gastric Secretion and Various Ulceration Models in Rats(Pharmacological,Chemical)

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• Bis[2-(E-2-alkenoylaminoethyl)] disulfides (I) and 2-(E-2-alkenoylamino)ethyl carbamoylmethyl sulfides (II) with various alkenyl chain lengths were synthesized and their inhibitory effects on gastric secretion in rats were compared. There was a relationship between the alkenyl chain length of a series of sulfide derivatives (II) and their biological activities (C10 and C11 alkenyl derivatives were the most effective compounds). On the other hand, variation of the alkenyl chain length did not affect the anti-ulcerogenic activity of the disulfide derivatives (1). The derivatives (II) showed stronger biological activity than (I) when the same alkenyl group was present in both. The administration of 2-(E-2-decenoylamino)ethyl carbamoylmethyl sulfide (II-5) or 2-(E-2-undecenoylamino)ethyl carbamoylmethyl sulfide (II-6) at a dose of 20mg/kg (i.p.) caused significant inhibition of various experimental ulcerations caused by stress, aspirin and HCl-ethanol. Oral administration of both acetamides (II-5,II-6) also caused 50-60% inhibition of ulceration in the water-immersion stress model at a dose of 20mg/kg, although the activity was not as strong as that after i.p. injection. An improvement in anti-ulcerogenic activity was observed when acetamides were administered as a suspension in 10%, HCO-60. Both acetamides (II-5, II-6) caused a dosedependent decrease of the ulcer index of restrained and water-immersion stress-loaded rats in the dosage range from 0.5mg/kg p.o. to 5mg/kg p.o. The lethal dose 50% values (LD_<50>) for both acetamides were over 8g/kg (p.o. or i.p.).

• 公益社団法人日本薬学会の論文
• 1987-11-25

著者

• 横山 和正

  Central Research Laboratory, Green Cross Corporation

• 横山 和正

  ミドリ十字、中研

• 辻川 和丈

  阪大薬

• 辻川 和丈

  Faculty of Pharmaceutical Sciences, Osaka University

• 三村 務

  Faculty of Pharmaceutical Sciences, Osaka University

• 岡部 勝

  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

• 中島 博志

  Faculty of Pharmaceutical Sciences, Osaka University

• KOHDA Isao

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

• 中島 博志

  Faculty Of Pharmaceutical Sciences Osaka University

• 三村 務

  大阪大学薬学部

• 岡部 勝

  大阪大薬学部

• 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

• 内藤 洋一郎

  Central Research Laboratories, Green Cross Corporation

• 深谷 力

  Central Research Laboratories, Green Cross Corporation

• 岡部 勝

  大阪大学 薬

• 横山 和正

  Central Research Laboratories The Green Cross Corporation

• 甲田 伊佐男

  Green Cross Corp. Osaka Jpn

• 内藤 洋一郎

  Central Research Laboratories Green Cross Corporation:department Of Agricultural Chemistry Faculty O

• 辻川 和丈

  Faculty of Pharmaceutical Sciences, Okayama University

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