Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents

…, Q Sun, Q Wu, P Sun, Y Zhang, X Yang, Y Jiang…

Index: Liu, Ping; Zhu, Shaolong; Li, Peng; Xie, Weijie; Jin, Yongsheng; Sun, Qingyan; Wu, Qiuye; Sun, Peng; Zhang, Yingjun; Yang, Xiaohong; Jiang, Yuanying; Zhang, Dazhi Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 11 p. 3261 - 3265

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Citation Number: 22

Abstract

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 ...