749200-87-1Relevant articles and documents
Triazole alcohol antifungal compound with piperidine oxadiazole side chain and preparation method for compound and application of compound
-
Paragraph 0110; 0111, (2016/10/07)
The invention relates to the medical technical field and provides 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(piperidine oxadiazole side chain substituted)-2-propanol compounds in one category. The compound comprises cis-trans-isomers thereof and any mixtures in the forms or pharmaceutical salts thereof. The chemical structural formula of the compound is represented by a formula (I). The invention further provides a preparation method for the compound and an application of the compound in preparing antifungal drugs. From an antifungal experiment, the compound provided by the invention has a very strong antifungal effect on various superficial fungi and deep fungi. Compared with existing clinically applied antifungal drugs such as fluconazole, the compound has the advantages of being efficient, low in toxicity and wide in antifungal spectrum, has relatively good activity on fluconazole drug-resistant bacteria and can be used for preparing antifungal drugs. The formula is shown in the description.
Discovery of highly potent triazole antifungal agents with piperidine-oxadiazole side chains
He, Xiaomeng,Jiang, Yan,Zhang, Yongqiang,Wu, Shanchao,Dong, Guoqiang,Liu, Na,Liu, Yang,Yao, Jianzhong,Miao, Zhenyuan,Wang, Yan,Zhang, Wannian,Sheng, Chunquan
, p. 653 - 664 (2015/04/27)
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. This journal is