高等学校化学学报

高等学校化学学报 ›› 2000, Vol. 21 ›› Issue (8): 1221.

• 论文 • 上一篇    下一篇

1-[2-(N-甲基-N-取代苄基)氨基-2-(4-叔丁基苯基)乙基]-1H-1,2,4-三唑类化合物的合成及抗真菌活性

冯志祥, 张万年, 周有骏, 吕加国, 朱驹, 李科   

  1. 第二军医大学药学院, 上海 200433
  • 收稿日期:1999-09-23 出版日期:2000-08-24 发布日期:2000-08-24
  • 通讯作者: 张万年(1948年出生),男,教授,博士生导师,从事药物化学研究.E-mail:Zhang wnk@online.sh.cn E-mail:Zhang wnk@online.sh.cn
  • 基金资助:

    国家自然科学基金(批准号:39770876);解放军“九五”重点课题(批准号:96z030)

Synthesis and Antifungal Activities of1-[2-(N-methyl-N- substituted- benzyl)amino-2-(4-tert- butylphenyl)ethyl]-1H- 1,2,4- triazoles

FENG Zhi-Xiang, ZHANG Wan-Nian, ZHOU You-Jun, LU Jia-Gou, ZHU Ju, LI Ke   

  1. Department of Medical Chemistry, College of Pharmacy, Second Military Medical University, Shanghai 200433, China
  • Received:1999-09-23 Online:2000-08-24 Published:2000-08-24

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被引次数

17

摘要： 根据氮唑类和苄胺类抗真菌药物的构效关系和作用机理,设计合成了23种1-[2-(N-甲基-N-取代苄基)氨基-2-(4-叔丁基苯基)乙基]-1H-1,2,4-三唑类化合物,其结构经元素分析、红外光谱及核磁共振谱分析证实.体外抑菌实验结果表明:目标化合物对常见的9种致病真菌均有一定活性,对浅表真菌活性优于深部真菌,其中化合物3,4,6,10,12,14和15对羊毛样小孢子菌具有较强的活性.

关键词: 三唑苄胺类化合物, 抗真菌活性, 合成, 构效关系

Abstract: Benzylamine and azole compounds respectively inhibit squelene exoxidase and cytochrome P450 monooxygenase which are two key enzymes in biosynthesis of fungal membrances. According to the structure-activitity relationships and antimycotic mechanism of azole and benzylamine compounds, we combined the feature of structure of those two kinds of compounds to design and synthesize twenty three 1-[2-(N-methyl-N-substituted-benzyl)amino-2-(4-tert-butylphenyl)ethyl] -1-H-1,2,4-triazoles. All of them were first reported and their structures were confirmed by elementary analysis, IRand 1H NMRspectra. The results of preliminary antifungal tests in vitro showed that all the compounds were active against the nine pathogenic fungi to some degrees. The activities against shallow fungi are greater than those of the deep ones. Compounds 3, 4, 6, 10, 12, 14 and 15 exhibited potent activities against microsporum canis.

Key words: 1,2,4-Triazolyl benzylamines, Fungicidal activity, Synthesis, Structure-activity relationship

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