Structure-Activity Relationships of 3-Methyl and 3,3-Dimethyl Analogs of 2-(2,4-Difluorophenyl)-3-(.OMEGA.)-substituted alkyl)sulfonyl-1-(1H-1,2,4-triazol-1-yl)-2-propanols.
説明
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.
収録刊行物
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- ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ
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ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ 44 (4), 785-792, 1996
公益社団法人 日本薬学会
