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Design, synthesis, and antifungal activities of novel triazole derivatives containing the benzyl group

Authors Xu K, Huang L, Xu Z, Wang Y, Bai G, Wu Q, Wang X, Yu S, Jiang Y

Received 26 September 2014

Accepted for publication 18 December 2014

Published 11 March 2015 Volume 2015:9 Pages 1459—1467

DOI https://doi.org/10.2147/DDDT.S74989

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 5

Editor who approved publication: Professor Shu-Feng Zhou


Kehan Xu,1,* Lei Huang,1,* Zheng Xu,2 Yanwei Wang,1,3 Guojing Bai,1 Qiuye Wu,1 Xiaoyan Wang,1 Shichong Yu,1 Yuanying Jiang1

1School of Pharmacy, Second Military Medical University, Shanghai, 2Shanghai Changzheng Hospital, Second Military Medical University, Shanghai, 3Number 422 Hospital of PLA, Zhanjiang, People’s Republic of China

*These authors contributed equally to this work

Abstract: In previous studies undertaken by our group, a series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols (1a–r), which were analogs of fluconazole, was designed and synthesized by click chemistry. In the study reported here, the in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi. Compounds 1a, 1q, and 1r showed the more antifungal activity than the others.

Keywords: triazole, synthesis, antifungal activity, CYP51

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