Synthesis in Vitro Antifungal Activities of Novel Triazole Antifungal Agent CS-758
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概要
- 論文の詳細を見る
Synthesis and in vitro antifungal activities of a novel triazole antifungal agent CS-758(former name, R-120758)are described. The minimum inhibitory concentrations(MICs) of a series of dioxane-triazole compounds related to R-102557 were examined. Variation of the length of the chain between the dioxane ring and the phenyl ring revealed that the linkage with two double bonds is the most preferable. When a cyano group was introduced to the C4 position on the benzene ring, MICs improved further. A fluorine atom was introduced to obtain CS-758. The MICs of CS-758 surpassed those of fluconazole and itraconazole against Candida, Aspergillus and Cryptococcus species. The precursor(E, E)-aldehyde was synthesized stereoselectively from 3-fluoro-4-methylbenzonitrile using the Horner-Wadsworth-Emmons reaction.
- 公益社団法人日本薬学会の論文
- 2001-12-01
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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Mori Makoto
Mechanical And Aerospace Engineering Tokyo Institute Of Technology
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Shimoji Y
Research Laboratories Sankyo Co. Ltd
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Mori Makoto
Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
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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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SEKI Shinobu
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.
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UCHIDA Takuya
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.
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SOMADA Atsushi
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.
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HARADA Yoshiko
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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SHIBAYAMA Takahiro
Pharmacokinetics and Drug Delivery Research Laboratories, Sankyo Co., Ltd.
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INOUE Shin-ichi
Pharmacokinetics and Drug Delivery Research Laboratories, Sankyo Co., Ltd.
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NAKAGAWA Akihiko
Pharmacokinetics and Drug Delivery Research Laboratories, Sankyo Co., Ltd.
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SETA Yasuo
Product Development 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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内田 丈士
Pharmaceutical Research Laboratory Kirin Brewery 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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Seki Shinobu
Medicinal Chemistry 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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Uchida Takuya
Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.
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Somada Atsushi
Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.
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Harada Yoshiko
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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Shimoji Y
Sankyo Co. Ltd. Tokyo Jpn
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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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Nakagawa Akihiko
Pharmacokinetics And Drug Delivery Research Laboratories Sankyo Co. Ltd.
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Shibayama Takahiro
Drug Metabolism & Pharmacokinetics Res. Laboratories Daiichi Sankyo Co. Ltd.
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Shibayama Takahiro
Research Laboratories Sankyo Co. Ltd
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Inoue Shin-ichi
Pharmacokinetics And Drug Delivery Research Laboratories Sankyo Co. Ltd.
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Konosu Toshiyuki
Medicinal Chemistry Res. Laboratories Ii Daiichi Sankyo Co. Ltd.
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