1-[2-(N-甲基-N-取代苄基)氨基-2-(2,4-二氯苯基)乙基]-1H-1,2,4-三唑类化合物的合成及抗真菌活性

1-[2-(N-甲基-N-取代苄基)氨基-2-(2,4-二氯苯基)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, 朱驹, 吕加国, 李科

第二军医大学药学院, 上海 200433

收稿日期:1999-10-19 修回日期:2000-02-09 出版日期:2000-12-15 发布日期:2000-12-15
通讯作者: 张万年*

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

Feng Zhixiang, Zhang Wannian^*, Zhou Youjun, Zhu Ju, Lu Jiaguo, Li Ke

Department of Medicinal Chemistry, College of Pharmacy, Second Military Medical University, Shanghai 200433

Received:1999-10-19 Revised:2000-02-09 Online:2000-12-15 Published:2000-12-15
Contact: Zhang Wannian*

摘要/Abstract

摘要：

根据氮唑类和苄胺类抗真菌化合物的构效关系和作用机理, 合成了22个1-[2-(N-甲基-N-取代苄基)氨基-2-(2, 4-二氯苯基)乙基]-1H-1, 2, 4-三唑类新化合物, 所有化合物经元素分析, 红外光谱和核磁共振谱确证结构。初步抑菌试验结果表明, 所有化合物对9种致病真菌具有不同程度的抑制作用。化合物2, 5, 6, 9, 10, 12, 13, 14 和18 对红色毛癣菌显示较强活性, 化合物1, 2, 5, 10, 15 和18对羊毛样小孢子菌抑制作用较强, 它们对该两种真菌的作用优于或相当于益康唑, 而化合物2和5对多种真菌均显示较强活性。

关键词: 三唑基苄胺, 抗真菌活性

Abstract: Based on the structure-activity relationships and antimycotic mechanism of azole and benzylamine antifungal compounds, twenty-two 1-[2-(N-methyl-N-substituted-benzyl)amino-2-(2,4-dichlorophenyl)ethyl]-1H-1,2,4-triazoles were designed and synthesized. All of them were first reported and their structures were confirmed by elementary analysis, IR and 1H NMR spectra. Results of preliminary antifungal tests in vitro show that all the compounds are active against the nine pathogenic fungi to some extent. Compounds 2, 5, 6, 9, 10, 12, 13, 14 and 18 exhibit great activities against Trichophyton rubrum, and compounds 1, 2, 5, 10, 15 and 18 are very active against Microsporum canis. Their antifungal activities against these two fungi are the same or more potent as compared with econazole; compounds 2 and 5 show great activity against many fungi.

Key words: Triazolyl benzylamines, Triazolyl benzylamines, Fungicidal activity, Fungicidal activity

Supporting: ^*Supported by the National Natural Science Foundation of China (39770876) and the Military “Nine Five” Key Assignment (96z030).

冯志祥, 张万年^*, 周有骏, 朱驹, 吕加国, 李科. 1-[2-(N-甲基-N-取代苄基)氨基-2-(2,4-二氯苯基)乙基]-1H-1,2,4-三唑类化合物的合成及抗真菌活性[J]. .

Feng Zhixiang, Zhang Wannian^*, Zhou Youjun, Zhu Ju, Lu Jiaguo, Li Ke. Synthesis and Antifungal Activities of 1-[2-(N-methyl-N-substituted-benzyl)amino-2-(2,4-dichlorophenyl)ethyl]-1H-1,2,4-triazoles[J]. .

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