Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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
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2001 Volume 49 Issue 2 Pages 173-182

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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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© 2001 The Pharmaceutical Society of Japan
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