Discovery of highly potent triazole antifungal derivatives by heterocycle-benzene bioisosteric replacement

Z Jiang, Y Wang, W Wang, S Wang, B Xu, G Fan…

Index: Jiang, Zhigan; Wang, Yan; Wang, Wenya; Wang, Shengzheng; Xu, Bo; Fan, Guorong; Dong, Guoqiang; Liu, Yang; Yao, Jianzhong; Miao, Zhenyuan; Zhang, Wannian; Sheng, Chunquan European Journal of Medicinal Chemistry, 2013 , vol. 64, p. 16 - 22

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Citation Number: 17

Abstract

On the basis of our previously discovered triazole antifungal lead compounds, heterocycle- benzene bioisosteric replacement was used to improve their pharmacokinetic profile. The designed new triazole derivatives have good antifungal activity toward a wide range of pathogenic fungi. Their binding mode with the target enzyme was clarified by molecular docking. The MIC value of the highly potent compound 8f against Candida albicans, ...