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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   

  1. 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*

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

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