Studies on Antiulcer Agents. II. Synthesis and Antiulcer Activity of Phenylpropanol Derivatives

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Other Title
  • 抗潰瘍剤の研究(第2報)Phenylpropanol誘導体の合成と抗潰瘍作用
  • 抗潰瘍剤の研究-2-Phenylpropanol誘導体の合成と抗潰瘍作用
  • コウ カイヨウザイ ノ ケンキュウ 2 Phenylpropanol ユウドウ

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Description

It was found that γ-irigermanal, obtained from the methanol extract of root of Iris germanica, exhibited a potent antiulcer activity. Therefore, this compound was selected as a lead-compound, and related compounds were synthesized and tested for antiulcer activities. It was found that (±) ethyl 2-[2-(3-hydroxypropyl)-4-oxocyclohexylidene]-propionate (1) had excellent antiulcer activities. Then phenylpropanol derivatives, obtained by changing from cyclohexane ring of 1 to benzene ring, were synthesized and tested for antiulcer activities in order to study structure-activity relationships. As a result, (±) ethyl 2-[2-(3-hydroxypropyl)-4, 5-dimethoxyphenyl] propionate (2b) and (±) 3-[2-(3-hydroxypropyl)-4, 5-dimethoxyphenyl]-2-butanone (5) were shown to have antiulcer activities.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 114 (12), 995-1004, 1994

    The Pharmaceutical Society of Japan

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