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目的:1[2(N甲基N取代苄基)氨基2(2,4二氟苯基) 乙基]1H1,2 ,4三唑类化合物的合成及抗真菌活性研究。方法:通过付克反应、三唑烷基化、酮亚胺还原和Leuckart 反应,得到关键中间体,然后通过N烷基化反应制得目标化合物,并用二倍稀释法测定了体外抑菌活性。结果:合成了23 个1[2(N甲基N取代苄基) 氨基2(2,4二氟苯基)乙基]1H1 ,2,4三唑类化合物,均为首次报道。所有目标化合物对8 种致病真菌均有不同程度的抗真菌活性。大部分化合物对Candida.albicans 和Candida.parapsilosis 的抗菌活性明显高于布替萘芬,其中1 ,2 ,6 ,13,14 ,19 对Candida.albicans 的抗菌活性是益康唑的8~32 倍,2,13 对Cryptococcu.neoformans 的抗菌活性是布替萘芬的4~8 倍,是益康唑64 ~128 倍。所有化合物对Microsporum .canis 的抗菌活性均高于或相当于益康唑。结论:其中一些化合物显示了较强抗真菌的活性,值得进一步研究
Purpose: 1 2 (N methyl N substituted benzyl) amino 2 (2, 4 - difluorophenyl) ethyl] 1 H 1, 2, 4 triazole compounds Synthesis and antifungal activity. Methods: Key intermediates were obtained by Friedel-Crafts reaction, triazoles alkylation, ketimine reduction and Leuckart reaction, and then the target compounds were obtained by N-alkylation. The in vitro antibacterial activity active. Results: A total of 23 1 [2 (N methyl N substituted benzyl) amino 2 (2,4 difluorophenyl) ethyl] 1 H 1, 2, 4 three Azoles, are the first reported. All the target compounds have different degrees of antifungal activity against the eight pathogenic fungi. The antibacterial activity of most of the compounds against Candida.albicans and Candida.parapsilosis was significantly higher than that of butenafine, of which 1,26, 13,14 and 19 were 8 ~ 32 times more active against Candida.albicans , 2,13 antibacterial activity of Cryptococcu.neoformans is 4-8 times of butenafine, is eupazole 64 to 128 times. The antimicrobial activity of all compounds against Microsporum canis was higher than or comparable to that of econazole. Conclusion: Some of these compounds show strong antifungal activity and deserve further study