4-(Benzoylindolizinyl)butyric Acids ; Novel Nonsteroidal Inhibitors of Steroid 5α-Reductase. III.^<1)>

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概要

• 論文の詳細を見る

• 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 inhibitiory 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.

• 公益社団法人日本薬学会の論文
• 2001-07-01

著者

• Tanaka H

  Faculty Of Pharmacy Meijo University

• Okada S

  School Of Pharmaceutical Sciences University Of Shizuoka

• 岡田 昌二

  静岡県立大学薬学部放射薬品学教室

• 岡田 昌二

  静岡県大 薬

• Okada S

  Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Tanaka H

  Department Of Agricultural Chemistry Faculty Of Agriculture Utsunomiya University

• Tanaka H

  Department Of Bioresources Chemistry Faculty Of Agriculture Okayama University

• Tanaka H

  Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• 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.

• 岡田 昌二

  静岡県大

• Toyama Hirohide

  Institute For Chemical Research Kyoto University

• Tanaka Haruyuki

  Chemical Branch Faculty Of Engineering And Kansai University High Technology Research Center Kansai

• Sawada Yuki

  Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Sawada Kozo

  Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Tanaka Hiroyoki

  Faculty Of Pharmaceutical Sciences Kyushu University

• Kuroda A

  Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Sawada K

  Kobe Pharmaceutical University

• Kuroda Akio

  Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Okada Satoshi

  Exploratory Research Laboratories Fujiawa Pharmaceutical Co. Ltd.

• Watanabe Shinya

  Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Tanaka Hirokazu

  Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd. :(present Address)external Scient

• Tanaka Hirokazu

  Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• TANAKA Hiromi

  Department of Physics Faculty of Education, Saga University

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