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| 新型1,2,3,4-四氢异喹啉类化合物的合成及抗真菌活性研究 |
| 朱驹,周有骏,吕加国,李耀武,郑灿辉,陈军,蒋庆锋 |
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| (第二军医大学药学院药物化学教研室,上海,200433) |
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| 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。 |
| 关键词: 四氢异喹啉类；抗真菌药 羊毛甾醇14α-去甲基化酶? |
| DOI：10.3724/SP.J.1008.2006.01299 |
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| 基金项目: |
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| Synthesis of novel 1, 2, 3, 4-tetrahydroisoquinolines and study of their anti-fungal activities? |
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| Abstract: |
| 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. |
| Key words: tetrahydroisoquinolines anti-fungal agents lanosterol 14α-demethylase? |
