Structure-Activity Relationships of 3-Methyl and 3,3-Dimethyl Analogs of 2-(2,4-Difluorophenyl)-3-(ω-substituted alkyl)sulfonyl-1-(1H-1,2,4-triazol-1-yl)-2-ipropanols

概要

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3-Methyl and 3,3-dimethyl analogs of 2-(2,4-difluorophenyl)-3-(ω-substituted alkyl)sulfonyl-1-(1H-1,2,4-triazol-1-yl)-2-propanols were synthesized and evaluated for their antifungal activites against Candida aldicans and Aspergillus fummigatus. The 3,3-dimethyl analogs were found to have more potent activity both in vitro and in vivo than the corresponding 3-mono-methyl analogs. The prophylactic efficacy of the lead compounds against murine systemic candidiasis and aspergillosis was improved signifcantly by dimethylation of the 3-position.
公益社団法人日本薬学会の論文
1996-04-15