Synthesis of Tricyclic Compounds as Steroid 5α-Reductase Inhibitors
スポンサーリンク
概要
- 論文の詳細を見る
A series of 4-phenoxybutyric acid derivatives attached to a tricyclic skelton were prepared and evaluated as 5α-reductase inhibitors. Structure activity relationships for these compounds in terms of rat epididymls (type 2)5α-reductase inhibitory activities reveal that 1) the substitution pattern at the 11-position of dibenz[b, e]oxepin influenced potency, 2) higher lipophilicity of the tricylic skeleton improved potency, whereas the existence of a basic nitrogen atom in this skeleton was detrimental to potency, and 3) isobutyl substitution at the 8 position of the azepine skelton was tolerated. Among the tricyclic compounds studied, 4-[3-[5-benzyl-8-(2-methyl)propyl-10,11-dihydrodibenz[b, f]azepine-2-carboxamido]phenoxy]butyric adid (26) was the most potent inhibitor of rat type 2 5α-reductase at 0.1μM.
- 公益社団法人日本薬学会の論文
- 2000-04-01
著者
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石井 昭男
協和発酵医薬研
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ISHII Akio
Toxicological Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
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KISHIBAYASHI Nobuyuki
Drug Development Research Laboratories, Pharmaceutical Research Institute, Kyowa Kogyo Co., Ltd.
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ISHII AKIO
Pharmaceuticals Research Laboratory, Kyowa Hakko Kogyo Co., Ltd.
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NONAKA Hiromi
Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Company
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Nonaka Hiromi
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Ishii A
Drug Development Research Laboratories Pharmaceutical Research Institute Kyowa Kogyo Co. Ltd.
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Ishii Akio
Pharmaceuticals Research Laboratory Kyowa Hakko Kogyo Co. Ltd.
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Kase Hiroshi
(present Address)kyowa Hakko Kogyo Co. Ltd.
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TAKAMI Hitoshi
(Present address) Kyowa Hakko Kogyo Co., Ltd.,
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KISHIBAYASHI Nobuyuki
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.,
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KUMAZAWA Toshiaki
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.,
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Takami H
(present Address) Kyowa Hakko Kogyo Co. Ltd.
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Kumazawa Toshiaki
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Kishibayashi N
Drug Development Research Laboratories Pharmaceutical Research Institute Kyowa Kogyo Co. Ltd.
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石井 昭男
協和発酵工業(株)医薬研究所
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ISHII Akio
Toxicological Research Laboratories Kyowa Hakko Kogyo Co., Ltd.
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Ishii Akio
Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
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