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Issue 4, 2015
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Discovery of highly potent triazoleantifungal agents with piperidine-oxadiazole side chains

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Abstract

Due to increasing incidence and mortality of invasive fungal infections, discovery and development of new generations of antifungal agents represents a challenging task. On the basis of our previously reported triazole-benzyloxypiperidinyl lead compound, a series of novel triazole antifungal agents containing piperidine-oxadiazole side chains were rationally designed and synthesized. Most of the target compounds showed excellent inhibitory activity against clinically important fungal pathogens. In particular, compounds 6g (MIC = 0.031 μg mL−1) and 11b (MIC = 0.016 μg mL−1) were highly active against Candida albicans including fluconazole-resistant strains. Moreover, they showed inhibitory activity against hyphal formation with low toxicity, which were promising leads for further development.

Graphical abstract: Discovery of highly potent triazole antifungal agents with piperidine-oxadiazole side chains

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Publication details

The article was received on 07 Nov 2014, accepted on 23 Dec 2014 and first published on 24 Dec 2014


Article type: Concise Article
DOI: 10.1039/C4MD00505H
Med. Chem. Commun., 2015,6, 653-664

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    Discovery of highly potent triazoleantifungal agents with piperidine-oxadiazole side chains

    X. He, Y. Jiang, Y. Zhang, S. Wu, G. Dong, N. Liu, Y. Liu, J. Yao, Z. Miao, Y. Wang, W. Zhang and C. Sheng, Med. Chem. Commun., 2015, 6, 653
    DOI: 10.1039/C4MD00505H

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