摘要
目的研究具有叔丁基结构的三唑醇类化合物的抗真菌活性以及各种4-(取代苄基)哌嗪侧链的引入对该类化合物抗真菌活性的影响。方法设计合成了13个未见文献报道的目标化合物,所有化合物结构均经1H-NMR谱确证,部分经过IR、MS确证;选择8种真菌为实验菌株,测定其体外抗真菌活性。结果所有化合物对8种真菌均有一定的抑制作用。其中,Ⅲ7的抑菌活性优于氟康唑。结论引入叔丁基和哌嗪侧链设计的目标化合物都具有抗真菌活性,侧链取代基的电性效应和立体化学特征的改变对该类化合物的抑菌活性有一定的影响。
Aim To study the antifungal activity of the triazole derivatives bearing the side chain containing t-butyl and the 4-（substituted benzyl）-piperazin and to compare their activities to those of fluconazole and itraconazole. Methods According to the structure of fluconazole, thirteen title compounds were designed and synthesized. All of them were confirmed by ^1H-NMR and parts of them were confirmed by IR, MS spectra. The MIC80 of all the title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards （NCCLS） using the RPMI 1640 test medium. Results All of the title compounds were reported firstly. The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent. Ⅲ7 was better than fluconazole in vit- ro .Conclusion The tide compounds with t-butyl and piperazine substituents have antifungal activities. Electrical property and stereochemistry may be important to the antifungal activities for the title compounds in vitro.
出处
《中国药物化学杂志》
CAS
CSCD
2006年第4期208-213,共6页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(30271542)
全军医药卫生科研基金项目(01MA156)
上海市科委科研项目(034319225)
关键词
药物化学
化合物制备
化学合成
叔丁基
三唑
体外抗真菌活性
medicinal chemistry
compound preparation
chemical synthesis
t-butyl
triazole
antifungal activity in vitro
