Optically Active Antifungal Azoles. V. Synthesis and Antifungal Activity of Stereoisomers of 3-Azolyl-2-(substituted phenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanols
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概要
- 論文の詳細を見る
The (2S, 3S)-, (2R, 3S)- and (2S, 3R)-stereoisomers of (2R, 3R)-3-azolyl-2-(substituted phenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanols [(2R, 3R)-1a-d] were prepared and evaluated for antifungal activity against Candida albicans in vitro and in vivo to clarify the relationships between stereochemistry and biological activities. The results revealed that the in vitro antifungal activity in each set of the four stereoisomers [(2R, 3R)-, (2S, 3S)-, (2R, 3S)- and (2S, 3R)-1a-d] definitely paralleled the in vivo antifungal activity against candidosis in mice, and the order of potency was (2R, 3R)≫(2R, 3S)≥(2S, 3S)≥(2S, 3R).In addition, the four stereoisomers in each set were assessed for sterol biosynthesis-inhibitory activities in C. albicans and rat liver. The (2R, 3R)-isomer was found to exert a strong and selective inhibitory effect on the sterol synthesis in C. albicans as compared with that in rat liver.
- 公益社団法人日本薬学会の論文
- 1995-03-15
著者
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伊藤 克己
Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries
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Tasaka A
Medicinal Chemistry Research Laboratories Pharmaceutical Research Division: Takeda Chemical Industri
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田坂 昭弘
Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries
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Tasaka Akihiro
Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries
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Itoh K
Medicinal Chemistiy Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industr
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Itoh K
Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries
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林 良吾
Pharmaceutical Research Laboratory III, Pharmaceutical Research Division, Takeda Chemical Industries
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小此木 研二
Pharmaceutical Research Laboratory III, Pharmaceutical Research Division, Takeda Chemical Industries
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北崎 智幸
Pharmaceutical Research Laboratories III, Pharmaceutical Research Division, Takeda Chemical Industri
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廣江 克彦
Pharmaceutical Research Laboratories Iii Pharmaceutical Researh Division Takeda Chemical Industries
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小此木 研二
Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries
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Itoh Kinuyo
Department Of Materials Chemistry & Frontier Research Center Graduate School Of Engineering. Osa
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Itoh Kunihiko
Dept. Pharmaceutical Sciences Akita University
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Hayashi R
Pharmacology Research Laboratories Ii Pharmaceutical Research Division Takeda Chemical Industries Lt
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土森 登
Pharmaceutical Research Laboratories III, Pharmaceutical Researh Division, Takeda Chemical Industrie
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土森 登
Pharmaceutical Research Laboratories Iii Pharmaceutical Researh Division Takeda Chemical Industries
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Kitazaki T
Pharmaceutical Research Division Takeda Pharmaceutical Company Limited
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北崎 智幸
Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries
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北崎 智幸
Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited
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