Synthesis of 1,2,3,4-Tetrahydro-β-carboline Derivatives as Hepatoprotective Agents. I. Dithiocarbamates of Several α-Amino Acids(Medicinal Chemistry,Chemical)

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概要

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• A series of dithiocarbamates of α-amino acids was synthesized and tested for hepatoprotective activity against CCl_4-induced liver damage in mice. Reaction of the amino acids (2,4, 6 and 8) with carbon disulfide followed by methylation gave the corresponding dithiocarbamates. Among the compounds synthesized, the β-carboline derivative (9a) exhibited remarkable hepatoprotective activity. The oxa analogues (9b-d) with respect to the dithiocarbamate group of 9a were also prepared. The activity of 9a-d decreased in the following order: dithiocarbamate (9a)>S-methyl thiocarbamate (9b)>O-methyl thiocarbamate (9c)>carbamate (9d). The structure-activity relationships are discussed.

• 社団法人日本薬学会の論文
• 1987-07-25

著者

• 石田 昭彦

  Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.

• 雑賀 豊

  Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 飯島 郁夫

  Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 宮城島 利一

  Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 大石 篤郎

  Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 松本 守

  Safety Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 松岡 雄三

  Safety Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 大石 篤郎

  Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.

• 松本 守

  Safety Research Laboratory Tanabe Seiyaku Co. Ltd.

• 宮城島 利一

  Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.

• 飯島 郁夫

  Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.

• 松岡 雄三

  Biological Research Laboratory:tanabe Seiyaku Co. Ltd.

• 雑賀 豊

  Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.

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