Xie Fei, Ni Tingjunhong, Zhao Jing, Pang Lei, Li Ran, Cai Zhan, Ding Zichao, Wang Ting, Yu Shichong, Jin Yongsheng, Zhang Dazhi, Jiang Yuanying
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China.
School of Pharmacy, Fujian University of Traditional Chinese Medicine, 1 Yueyang Road, Fuzhou 350112, China.
Bioorg Med Chem Lett. 2017 May 15;27(10):2171-2173. doi: 10.1016/j.bmcl.2017.03.062. Epub 2017 Mar 23.
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.
设计并合成了29种瑞伏康唑和艾沙康唑的新型三唑类似物。大多数化合物对8种真菌分离株表现出强效的体外抗真菌活性。特别是，化合物a10、a13和a14对所有测试真菌表现出与瑞伏康唑相当或更优的抗真菌活性。构效关系研究表明，用氟苯基异恶唑取代瑞伏康唑的4-氰基苯基噻唑部分可得到更有效、更广谱的新型抗真菌三唑类化合物。
