Optically Active Antifungal Azoles. X. Synthesis and Antifungal Activity of N-[4-(Azolyl)phenyl]- and N-[4-(Azolylmethyl)phenyl]-N'-[(1R, 2R)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-azolones
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概要
- 論文の詳細を見る
New optically active antifungal azoles, N-[4-(azolyl)phenyl]- and N-[4-(azolylmethyl)phenyl]-N'-[(1R, 2R)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]azolones (1,2,3), were prepared in a stereocontrolled manner. Compounds 1-3 showed strong antifungal activity against Candida albicans in vitro. Among them, the imidazolidinones 3 showed a broad antifungal spectrum in vitro as well as potent in vivo activity against candidiasis and aspergillosis in mice. The imidazolidinones (3i, j, k) having 1H-1,2,3-triazol-1-yl, 2H-2-tetrazolyl and 1H-1-tetrazolyl moieties were found to exert strong protective effect against aspergillosis.
- 公益社団法人日本薬学会の論文
- 2000-12-01
著者
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Yamada Makiko
San-ei Gen F.f.i. Inc.
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Tasaka A
Medicinal Chemistry Research Laboratories Pharmaceutical Research Division: Takeda Chemical Industri
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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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Yamada M
Pharmaceutical Research Division Takeda Pharmaceutical Company Limited
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Yoshida M
Tohoku Univ. Sendai Jpn
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Ichikawa Takashi
Pharmaceutical Research Division Takeda Pharmaceutical Company Limited
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KITAZAKI Tomoyuki
Medicinal Chemistry Research Laboratories II, Pharmaceutical Research Division, Takeda Chemical Indu
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HAYASHI Ryogo
Pharmacology Research Laboratories II, Pharmaceutical Research Division, Takeda Chemical Industries,
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OKONOGI Kenji
Research Management Department, Pharmaceutical Research Division, Takeda Chemical Industries, Ltd.
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ICHIKAWA Takashi
Discovery Research Laboratories V, Pharmaceutical Discovery Research Division Takeda Chemical Indust
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MATSUSHITA Yoshihiro
Discovery Research Laboratories V, Pharmaceutical Discovery Research Division Takeda Chemical Indust
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HOSONO Hiroshi
Medicinal Chemistry Research Laboratories, Pharmaceutical Research Division Takeda Chemical Industri
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ITOH Katsumi
Discovery Research Laboratories V, Pharmaceutical Discovery Research Division Takeda Chemical Indust
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TASAKA Akihiro
Medicinal Chemistry Research Laboratories Pharmaceutical Research Division
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Ichikawa T
Pharmaceutical Research Division Takeda Pharmaceutical Company Limited
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Itoh K
Graduate School Of Pharmaceutical Sciences Chiba University:nisshin Seifun Group Inc.
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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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Okonogi K
Pharmacology Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries Ltd
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Hosono H
Medicinal Chemistry Research Laboratories Pharmaceutical Research Division: Takeda Chemical Industri
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Kitazaki T
Pharmaceutical Research Division Takeda Pharmaceutical Company Limited
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Hosono Hiroshi
Medicinal Chemistry Research Laboratories Pharmaceutical Research Division: Takeda Chemical Industries, Ltd.,
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