New Antifungal 1, 2, 4-Triazoles with Difluoro(substituted sulfonyl)methyl Moiety

Hiromichi ETO; Yasushi KANEKO; Sunao TAKEDA; Minoru TOKIZAWA; Susumu SATO; Kouiti YOSHIDA; Setsuo NAMIKI; Masaki OGAWA; Kazuki MAEBASHI; Kazuya ISHIDA; Masaru MATSUMOTO; Takemitsu ASAOKA

doi:10.1248/cpb.49.173

Regular Articles

New Antifungal 1, 2, 4-Triazoles with Difluoro(substituted sulfonyl)methyl Moiety

Hiromichi ETO, Yasushi KANEKO, Sunao TAKEDA, Minoru TOKIZAWA, Susumu SATO, Kouiti YOSHIDA, Setsuo NAMIKI, Masaki OGAWA, Kazuki MAEBASHI, Kazuya ISHIDA, Masaru MATSUMOTO, Takemitsu ASAOKA

著者情報

Hiromichi ETO
Central Research Labs., SS Pharmaceutical Co., Ltd.
Yasushi KANEKO
Central Research Labs., SS Pharmaceutical Co., Ltd.
Sunao TAKEDA
Central Research Labs., SS Pharmaceutical Co., Ltd.
Minoru TOKIZAWA
Central Research Labs., SS Pharmaceutical Co., Ltd.
Susumu SATO
Central Research Labs., SS Pharmaceutical Co., Ltd.
Kouiti YOSHIDA
Central Research Labs., SS Pharmaceutical Co., Ltd.
Setsuo NAMIKI
Central Research Labs., SS Pharmaceutical Co., Ltd.
Masaki OGAWA
Central Research Labs., SS Pharmaceutical Co., Ltd.
Kazuki MAEBASHI
Central Research Labs., SS Pharmaceutical Co., Ltd.
Kazuya ISHIDA
Central Research Labs., SS Pharmaceutical Co., Ltd.
Masaru MATSUMOTO
Central Research Labs., SS Pharmaceutical Co., Ltd.
Takemitsu ASAOKA
Central Research Labs., SS Pharmaceutical Co., Ltd.

キーワード: antifungal, 1,2,4-triazole, difluoro(substituted sulfonyl)methyl derivative

ジャーナルフリー

2001 年 49 巻 2 号 p. 173-182

DOI https://doi.org/10.1248/cpb.49.173

詳細

抄録

New 1, 2, 4-triazoles (2) having a difluoro(substituted sulfonyl)methyl moiety were designed and synthesized via α, α-difluoro-α-(substituted thio)acetophenones (3). Compounds (2) showed potent antifungal activities against C. albicans, C. krusei, A. flavus and A. fumigatus in vitro and against C. albicans in vivo for oral and i.v. administrations. Especially, (−)-2a, (−)-2b and (−)-2d showed potent antifungal activities.

責任著者(Corresponding author)

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