期刊
MEDCHEMCOMM
卷 6, 期 4, 页码 653-664出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c4md00505h
关键词
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资金
- National Natural Science Foundation of China [81222044]
- Science and Technology Commission of Shanghai Municipality [13431900301]
- 863 Hi-Tech Program of China [2014AA020525]
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 mu g mL(-1)) and 11b (MIC = 0.016 mu g 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.
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