具有二氟（取代磺酰基）甲基部分的新型抗真菌1,2,4-三唑类化合物。

New antifungal 1,2,4-triazoles with difluoro(substituted sulfonyl)methyl moiety.

作者信息

Eto H, Kaneko Y, Takeda S, Tokizawa M, Sato S, Yoshida K, Namiki S, Ogawa M, Maebashi K, Ishida K, Matsumoto M, Asaoka T

机构信息

Central Research Labs., SS Pharmaceutical Co., Ltd., Narita, Chiba, Japan.

出版信息

Chem Pharm Bull (Tokyo). 2001 Feb;49(2):173-82. doi: 10.1248/cpb.49.173.

DOI:10.1248/cpb.49.173

PMID:11217105

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.

摘要

设计并合成了具有二氟（取代磺酰基）甲基部分的新型1,2,4-三唑（2），其通过α,α-二氟-α-（取代硫代）苯乙酮（3）制备。化合物（2）在体外对白色念珠菌、克鲁斯念珠菌、黄曲霉和烟曲霉显示出强效抗真菌活性，在体内口服和静脉注射时对白色念珠菌也有活性。特别是，（-）-2a、（-）-2b和（-）-2d表现出强效抗真菌活性。