4-(1-Benzoylindol-3-yl)butyric Acids and FK143 : Novel Nonsteroidal Inhibitors of Steroid 5α-Reductase (II)
スポンサーリンク
概要
- 論文の詳細を見る
A novel series of indolebutyric acids with varying benzoyl substituents were synthesized to develop nonsteroidal inhibitors of steroid 5α-reductase. We previously reported the discovery of a novel nonsteroidal 5α-reductase inhibitor, FR119680,which had an IC_<50> value of 5.0 nM against the rat prostatic enzyme. However, this compound was not strongly active against the human prostatic enzyme. By further study of the structure-activity relationships we succeeded in producing the strongly active compound, FK143,4-[3-[3-[bis(4-isobutylphenyl)-methylamino]benzoyl]-1H-indol-1-yl]butyric acid, with an IC_<50> value of 1.9 nM against the human enzyme. FK143 also has in vivo inhibitory activity against the castrated young rat model and it should therefore be an extremely useful agent for the treatment of benign prostatic hyperplasia.
- 公益社団法人日本薬学会の論文
- 1999-04-15
著者
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Tanaka H
Faculty Of Pharmacy Meijo University
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Okada S
School Of Pharmaceutical Sciences University Of Shizuoka
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岡田 昌二
静岡県立大学薬学部放射薬品学教室
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岡田 昌二
静岡県大 薬
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Okada S
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Tanaka H
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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SAWADA Kozo
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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OKADA Satoshi
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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SAWADA Yuki
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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TANAKA Hirokazu
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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HASHIMOTO Masashi
Exploratory Research Laboratories, Fujisawa Phamaceutical Co., Ltd.,
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岡田 昌二
静岡県大
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Toyama Hirohide
Institute For Chemical Research Kyoto University
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Tanaka Haruyuki
Chemical Branch Faculty Of Engineering And Kansai University High Technology Research Center Kansai
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Sawada Yuki
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Sawada Kozo
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Sawada K
Kobe Pharmaceutical University
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Hashimoto M
Exploratory Research Laboratories Fujisawa Phamaceutical Co. Ltd. :(present Address)tsukuba Research
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Hashimoto Masashi
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Okada Satoshi
Exploratory Research Laboratories Fujiawa Pharmaceutical Co. Ltd.
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Tanaka Hirokazu
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd. :(present Address)external Scient
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Tanaka Hirokazu
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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TANAKA Hiromi
Department of Physics Faculty of Education, Saga University
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