Design,synthesis, and in vitro evaluation of novel antifungal triazoles |
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| Authors: | Fei Xie Tingjunhong Ni Jing Zhao Lei Pang Ran Li Zhan Cai Zichao Ding Ting Wang Shichong Yu Yongsheng Jin Dazhi Zhang Yuanying Jiang |
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| Affiliation: | 1. Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China;2. School of Pharmacy, Fujian University of Traditional Chinese Medicine, 1 Yueyang Road, Fuzhou 350112, China;3. Center of New Drug Research, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China |
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| Abstract: | Twenty-nine novel triazole analogues of ravuconazole and isavuconazole were designed and synthesized. Most of the compounds exhibited potent in vitro antifungal activities against 8 fungal isolates. Especially, compounds a10, a13, and a14 exhibited superior or comparable antifungal activity to ravuconazole against all the tested fungi. Structure-activity relationship study indicated that replacing 4-cyanophenylthioazole moiety of ravuconazole with fluorophenylisoxazole resulted in novel antifungal triazoles with more effectiveness and a broader-spectrum. |
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| Keywords: | Isoxazole Triazole Antifungal activity Structure-activity relationship Synthesis |
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