4-(Benzoylindolizinyl)butyric Acids; Novel Nonsteroidal Inhibitors of Steroid 5.ALPHA.-Reductase. III.

DOI Web Site Web Site PubMed 2 Citations 52 References
  • 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.

Bibliographic Information

Other Title
  • 4-(Benzoylindolizinyl)butyric Acids: Novel Nonsteroidal Inhibitors of Steroid 5α-Reductase(3)
  • 4 Benzoylindolizinyl butyric Acids Novel Nonsteroidal Inhibitors of Steroid 5 アルファ Reductase 3

Search this article

Abstract

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.

Journal

Citations (2)*help

See more

References(52)*help

See more

Keywords

Details 詳細情報について

Report a problem

Back to top