Benzimidazole-5-sulfonamides as Novel Nonpeptide Luteinizing Hormone Releasing Hormone (LHRH) Antagonists : Minimization of Mechanism-Based CYP3A4 Inhibition
スポンサーリンク
概要
- 論文の詳細を見る
Herein we report the development of novel, potent and non-peptide luteinizing hormone releasing hormone (LHRH) antagonists. The optimization towards derivatives free from mechanism-based CYP3A4 inhibition is described. The identification of a main metabolite guided us towards structural modifications of the benzyl moiety, which resulted in significant improvements of the CYP3A4 profile, while maintaining potent LHRH antagonist activity.
- 社団法人日本薬学会の論文
- 2005-10-01
著者
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Yamamoto Mako
Research Center Kyoto Bayer Yakuhin Ltd.
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YAMAMOTO Noriyuki
Research Center Kyoto, Bayer Yakuhin, Ltd.
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Yamamoto Noriyuki
Research Center Kyoto Bayer Yakuhin Ltd.
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HASHIMOTO Kentaro
Research Center Kyoto, Bayer Yakuhin, Ltd.
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KATAOKA Mikayo
Research Center Kyoto, Bayer Yakuhin, Ltd.
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TATSUTA Miyuki
Research Center Kyoto, Bayer Yakuhin, Ltd.
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YASOSHIMA Kayo
Research Center Kyoto, Bayer Yakuhin, Ltd.
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YURA Takeshi
Research Center Kyoto, Bayer Yakuhin, Ltd.
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URBAHNS Klaus
Research Center Kyoto, Bayer Yakuhin, Ltd.
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GUPTA Jang
Research Center Kyoto, Bayer Yakuhin, Ltd.
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LI Yingfu
Research Center Kyoto, Bayer Yakuhin, Ltd.
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Li Yingfu
Research Center Kyoto Bayer Yakuhin Ltd.
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Gupta Jang
Research Center Kyoto Bayer Yakuhin Ltd.
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Yura Takeshi
Research Center Kyoto Bayer Yakuhin Ltd.
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Urbahns Klaus
Research Center Kyoto Bayer Yakuhin Ltd.
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Tatsuta Miyuki
Research Center Kyoto Bayer Yakuhin Ltd.
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Yasoshima Kayo
Research Center Kyoto Bayer Yakuhin Ltd.
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Kataoka Mikayo
Research Center Kyoto Bayer Yakuhin Ltd.
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Hashimoto Kentaro
Research Center Kyoto Bayer Yakuhin Ltd.
関連論文
- Inhibition of Syk Activity and Degranulation of Human Mast Cells by Flavonoids (Pharmacology)
- Benzimidazole-5-sulfonamides as Novel Nonpeptide Luteinizing Hormone Releasing Hormone (LHRH) Antagonists : Minimization of Mechanism-Based CYP3A4 Inhibition