(1-Benzylinodole-3-yl)alkanoic Acids : Novel Nonsteroidal Inhibitors of Steroid 5α-Reductase (I)
スポンサーリンク
概要
- 論文の詳細を見る
A novel series of indole-3-alkanoic acids with varied N-benzyl substituents were synthesized as nonsteroidal inhibitors of steroid 5α-reductase. The structure-activity relationship in this series were studied and the optimum carboxylic acid side chain was butyric acid. Furthermore, compounds with a diaryl substituent at the 1-position of the indole ring displayed strong inhibitory activities in vitro. Amongst these derivatives, 4-[1-(6,6-dimethyl-6H-dibenzo[b, d]pyran-3-yl)methylindol-3-yl]butyric acid (FR119680) displayed very high inhibitory activity in vitro against rat prostatic 5α-reductase (IC_<50>=5.0 nM) and good in vivo activity in the castrated young rat model.
- 公益社団法人日本薬学会の論文
- 1998-11-15
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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HIRAI Hideo
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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GOLDEN Patrick
Exploratory Research Laboratories, Fujisawa Pharmaceutical 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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Hirai Hideo
Exploratory Medicinal Sciences Pfizer Global Research And Development(pgrd)-nagoya Laboratories Pfiz
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Hirai Hideo
Faculty Of Pharmaceutical Sciences Tokushima Bunri University
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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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