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目的:以氟康唑为先导化合物,设计合成新的三唑醇类化合物,并研究其抗真菌活性。方法:引入异丙基及取代氨基侧链结构,合成一系列目标化合物,所有化合物结构均经MS1、H-NMR等谱确证;选择8种真菌为实验菌株,测定其体外抗真菌活性。结果:合成了15个目标化合物;所有化合物对所选真菌均表现出了一定的抑菌活性,其中化合物(6c),(6d),(6e),(6 f)和(6g)对除薰烟曲霉菌外的7种菌株都表现出了较好的抑菌活性。结论:取代氨基侧链结构的引入对目标化合物的抗菌活性有一定的影响,侧链为取代苄基活性较好,且取代苄基侧链越短,抑菌活性越好。
OBJECTIVE: To design and synthesize new triazole alcohols with fluconazole as the lead compound and study its antifungal activity. Methods: A series of target compounds were synthesized by the introduction of isopropyl and substituted amino side chains. The structures of all the compounds were confirmed by MS1 and H-NMR spectra. Eight kinds of fungi were chosen as experimental strains to test their antifungal activities in vitro. Results: Fifteen target compounds were synthesized. All the compounds showed some antibacterial activities against the selected fungi. Among them, compounds (6c), (6d), (6e), (6f) and Seven strains of Aspergillus fumigatus showed good antibacterial activity. CONCLUSION: The introduction of substituted amino side chain structure has certain effect on the antibacterial activity of the target compound. The side chain is better substituted benzyl, and the shorter substituted benzyl side chain, the better the antibacterial activity.