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Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents. 2008
Ping Liu, and
Shaolong Zhu, and
Peng Li, and
Weijie Xie, and
Yongsheng Jin, and
Qingyan Sun, and
Qiuye Wu, and
Peng Sun, and
Yingjun Zhang, and
Xiaohong Yang, and
Yuanying Jiang, and
Dazhi Zhang
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China.
A series of 1-(substituted biaryloxy)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl) propan-2-ol were synthesized and their antifungal activities were evaluated against eight human pathogenic fungi in vitro. Seventeen compounds showed activity 4- to 64-fold higher than voriconazole against Candida albicans. SAR clearly suggested that introduction of a biaryloxy side chain greatly enhanced the antifungal activity of triazole analogs against Candida species.
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