Synthesis of 1,2,3,4-Tetrahydro-β-carboline Derivatives as Hepatoprotective Agents. II. : Alkyl 1,2,3,4-Tetrahydro-β-carboline-2-carbodithioates(Medeicinal Chemistry,Chemical)
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概要
- 論文の詳細を見る
A large number of aikyl 1,2,3,4-tetrahydro-β-carboline-2-carbodithioates (2 and 5) with 3-hydroxycarbonyl and 3-hydroxymethyI groups were synthesized and tested for hepatoprotective activity against CCl_4-induced liver damage in mice. Structure-activity relationships were investigated. Lengthening of the alkyl group in 2 and 5 tends to adversely affect the activity. Both enantiomers of the methyl derivatives (2a and 5a), the most potent compounds in this series, were synthesized, and no difference in hepatoprotective activity was observed. Apparent neighboring group participation was observed in the treatment of 5a with base or acid, giving the cyclized product (6) or the rearranged products (7, 8, and 9).
- 公益社団法人日本薬学会の論文
- 1987-08-25
著者
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Matsumoto M
Osaka Medical Center For Cancer And Cardiovascular Diseases Osaka
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Matsumoto Misako
Department Of Immunology Osaka Medical Center For Cancer And Cardiovascular Diseases
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Ishida Akihiko
Organic Chemistry Research Laboratory Tanabe Seiyaku
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Matsumoto Mitsuharu
Takeda Chemical Industries Ltd. Pharmaceutical Research Division
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Matsuoka Y
Safety Research Laboratory And Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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Miyagishima T
Tanabe Seiyaku Co. Ltd. Saitama
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SAIGA Yutaka
Lead Optimization Research Laboratory, Tanabe Seiyaku Co., Ltd.,
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Saiga Y
Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.
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MATSUMOTO MAMORU
Safety Research Laboratory
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MATSUOKA YUZO
Safety Research Laboratory
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SAIGA YUTAKA
Organic Chemistry Research Laboratory
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MIYAGISHIMA TOSHIKAZU
Organic Chemistry Research Laboratory
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OH-ISHI TOKURO
Organic Chemistry Research Laboratory
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SHIGEZANE KEISUKE
Organic Chemistry Research Laboratory, Tanabe Seiyaku
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Shigezane K
Organic Chemistry Research Laboratory Tanabe Seiyaku
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Oh‐ishi T
Tanabe Seiyaku Co. Ltd. Saitama Jpn
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