title: New antifungal 1,2,4-triazoles with difluoro(substituted sulfonyl)methyl moiety.
abstract: New 1,2,4-triazoles (2) having a difluoro(substituted sulfonyl)methyl moiety were designed and synthesized via alpha,alpha-difluoro-alpha-(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.
authors.affiliation: Central Research Labs., SS Pharmaceutical Co., Ltd., Narita, Chiba, Japan. Hiromichi.Eto@ssp.co.jp
authors.forename: H
authors.initials: H
authors.lastname: Eto
authors.forename: Y
authors.initials: Y
authors.lastname: Kaneko
authors.forename: S
authors.initials: S
authors.lastname: Takeda
authors.forename: M
authors.initials: M
authors.lastname: Tokizawa
authors.forename: S
authors.initials: S
authors.lastname: Sato
authors.forename: K
authors.initials: K
authors.lastname: Yoshida
authors.forename: S
authors.initials: S
authors.lastname: Namiki
authors.forename: M
authors.initials: M
authors.lastname: Ogawa
authors.forename: K
authors.initials: K
authors.lastname: Maebashi
authors.forename: K
authors.initials: K
authors.lastname: Ishida
authors.forename: M
authors.initials: M
authors.lastname: Matsumoto
authors.forename: T
authors.initials: T
authors.lastname: Asaoka
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002175:Candida / Q000187:drug effects; D018360:Crystallography, X-Ray; D005461:Fluorine / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013045:Species Specificity; D013450:Sulfones / Q000737:chemistry*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D013450:Sulfones; D014230:Triazoles; D005461:Fluorine