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

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Keywords: antifungal, 1,2,4-triazole, difluoro(substituted sulfonyl)methyl derivative

JOURNAL FREE ACCESS

2001 Volume 49 Issue 2 Pages 173-182

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

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Abstract

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.

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