Synthesis and Antifungal Activities of R-102557 and Related Dioxane-Triazole Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
Novel triazole compounds with a dioxane ring were synthesized. Condensation of the diol precursor 10 with various aromatic aldehydes 11-13 under acidic conditions afforded a series of dioxane-triazole compounds 14-16. The antifungal activities of the compounds 14-16 were evaluated in vivo in mice infection models against Candida and Aspergillus species. High activities were seen for the derivatives with one or two double bond(s) and an aromatic ring substituted with an electron-withdrawing group in th side chain. Among the derivatives, R-102557 (16R : Ar=4-(2,2,3,3)-tetrafluoropropoxy)phenyl)showed excellent in vivo activities against Candida, As-pergillus and Cryptococcus species. It also showed high tolerance in a preliminary toxicity study in rats.
- 公益社団法人日本薬学会の論文
- 2000-05-01
著者
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中村 康彦
Department Of Formulation Research Dainippon Pharmaceutical Co. Ltd.
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Yasuda H
Biological Research Laboratories Sankyo Co. Ltd.
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Tajima Y
Saga Medical School Hospital Saga Jpn
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Kamai Yasuki
Biological Research Laboratories IV, Daiichi Sankyo Co., Ltd.
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Konosu Toshiyuki
Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd.
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OIDA Sadao
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.
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NAKAMURA Yoshie
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.
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SOMADA Atsushi
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.
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HARASAKI Tamako
Biological Research Laboratories, Sankyo Co., Ltd.
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FUKUOKA Takashi
Biological Research Laboratories, Sankyo Co., Ltd.
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OHYA Satoshi
Biological Research Laboratories, Sankyo Co., Ltd.
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YASUDA Hiroshi
Biological Research Laboratories, Sankyo Co., Ltd.
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Ohya S
Research Laboratories Sankyo Co. Ltd
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Ohya Satoshi
Biological Research Laboratories Sankyo Co. Ltd.
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Yasuda Hideyuki
Department Of Basic Research Lotte Central Laboratory Co. Ltd.
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Nakamura Yoshihide
Technical Department Fuji Chemical Industries Co. Ltd.
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Nakamura Y
Tohoku Pharmaceutical Univ. Sendai Jpn
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Oida Sadao
Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.
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Harasaki Tamako
Biological Research Laboratories Sankyo Co. Ltd.
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Kamai Y
Sankyo Co. Ltd. Tokyo
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Kamai Yasuki
Teikyo University Institute Of Medical Mycology
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Somada Atsushi
Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.
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TAJIMA Yawara
Medicinal Chemistry Research Laboratories Sankyo Co., Ltd.,
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TANAKA Teruo
Medicinal Chemistry Research Laboratories Sankyo Co., Ltd.,
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HABUKI Shinobu
Medicinal Chemistry Research Laboratories Sankyo Co., Ltd.,
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Habuki Shinobu
Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.
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Fukuoka Takashi
Research Laboratories Sankyo Co. Ltd
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Fukuoka T
Department Of Hygiene And Microbiology Faculty Of Veterinary Medicine Hokkaido University
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Nakamura Y
Department Of Pharmacognosy Tohoku Pharmaceutical University
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Fukuoka Takashi
Biological Research Laboratories Sankyo Co. Ltd.
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鴻巣 俊之
Medicinal Chemistry Res. Laboratories Ii Daiichi Sankyo Co. Ltd.
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Konosu Toshiyuki
Department Of Chemistry Faculty Of Science The University Of Tokyo
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Tanaka Teruo
Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.
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Konosu Toshiyuki
Medicinal Chemistry Res. Laboratories Ii Daiichi Sankyo Co. Ltd.
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