Synthetic Models Related to Furanocoumarin-CYP 3A4 Interactions. Comparison of Furanocoumarin, Coumarin, and Benzofuran Dimers as Potent Inhibitors of CYP3A4 Activity
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- Oda Kazuaki
- Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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- Yamaguchi Yuki
- Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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- Yoshimura Teruki
- Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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- Wada Keiji
- Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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- Nishizono Naozumi
- Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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説明
Furanocoumarin derivatives (dimers and monomers) present in commercially available grapefruit juice have the capacity to inhibit the activity of human CYP3A4. Such interactions are believed to result from the mechanism-based inhibition of CYP3A4 activity in the intestine. The aim of this work was to synthesize and test a series of dimers with a view to determining the relationship between structure and inhibitory activity and determining whether they might make suitable probes of CYP3A4 activity. We prepared a series of furanocoumarin, coumarin, and benzofuran derivatives that have inhibitory effects on the activity of human CYP3A4. A synthetic benzofuran dimer, which is more accessible than furanocoumarin dimers, exhibited activity against CYP3A4 comparable to that of furanocoumarin dimers.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 55 (9), 1419-1421, 2007
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204168145408
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- NII論文ID
- 110006379673
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 8878086
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDLサーチ
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