摘要
目的：设计合成新型四氢异喹啉类抗真菌化合物。方法：以3，4，5-三甲氧基苯乙胺为起始原料，经Pictet—Spengler反应、中和反应、取代反应、酸性裂解等反应合成目标化合物，并进行体外抗真菌活性研究。结果：设计合成了12个新型四氢异喹啉类化合物，12个目标化合物均为首次报道。所有目标化合物均有抗真菌活性，其中化合物6～8、10～12对4种测试菌的抗菌活性均强于或相当于氟康唑。结论：设计合成的目标分子是一类新型的抗真菌化合物。此类化合物具有进一步研究开发的价值。
Objective：To design and synthesize novel tetrahydroisoquinolines with anti-fungal activities. Methods： 3,4-dimethoxyphenylethylamine was taken as the template and the title compounds were synthesized through Pictet-Spengler reaction, neutralization reaction, substitution, hydrolysis, and acylation. Results： Twelve title compounds were obtained and all of them were firstly reported. Besides, all the target compounds had anti-fungal activities. The anti-fungal activities of compounds 6-8 and 10-12 were similar to or stronger than that of fluconazole＇ s. Conclusion： Title compounds obtained in this study belong to a new type of anti-fungal agent, which deserves further study.
出处
《第二军医大学学报》
CAS
CSCD
北大核心
2006年第12期1299-1303,共5页
Academic Journal of Second Military Medical University
基金
国家自然科学基金(30572257).~~
