4-(Benzoylindolizinyl)butyric Acids: Novel Nonsteroidal Inhibitors of Steroid 5α-Reductase(3)

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  • SAWADA Kozo
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • OKADA Satoshi
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • KURODA Akio
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • WATANABE Shinya
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • SAWADA Yuki
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • TANAKA Hirokazu
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.

書誌事項

タイトル別名
  • 4-(Benzoylindolizinyl)butyric Acids; Novel Nonsteroidal Inhibitors of Steroid 5.ALPHA.-Reductase. III.
  • 4 Benzoylindolizinyl butyric Acids Novel Nonsteroidal Inhibitors of Steroid 5 アルファ Reductase 3

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抄録

A novel series of indolizinebutyric acids with various benzoyl substituents was synthesized to develop nonsteroidal inhibitors of steroid 5α-reductase, and the structure-activity relationships in this series were studied. We previously reported the structure-activity relationships in a series of indolebutyric acids as well as the discovery of the novel nonsteroidal 5α-reductase inhibitor, FK143. We have now made other modifications to this compound to improve in vivo inhibitory activity. By altering the heterocyclic nucleus and changing the benzoyl substituent we have succeeded in identifying the strongly active compound, FK687, (S)-4-[1-[4-[[1-(4-isobutylphenyl)butyl]oxy]benzoyl]indolizin-3-yl]butyric acid, which displays strong in vitro inhibitory activity against the human enzyme and in vivo inhibitory activity against the castrated young rat model. This compound should be a useful agent for the treatment of benign prostatic hyperplasia.

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