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-(2,4-二氟苯基)乙基-1H-1,2,4-三唑类化合物的合成及抗真菌活性J. 药学学报, 1999, 34(12): 902-907.
引用本文: 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-(2,4-二氟苯基)乙基-1H-1,2,4-三唑类化合物的合成及抗真菌活性J. 药学学报, 1999, 34(12): 902-907.
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Feng Zhixiang, Zhang Wannian, Zhou Youjun Zhu Ju Lü Jiaguo , Li Ke, . SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF-1-2-(-N-METHYL-N-SUBSTITUTED-BENZYL)AMINO-2-(2,4-DIFLUOROPHENYL) ETHYL-1H-1,2,4-TRIAZOLESJ. Acta Pharmaceutica Sinica, 1999, 34(12): 902-907.
Citation: Feng Zhixiang, Zhang Wannian, Zhou Youjun Zhu Ju Lü Jiaguo , Li Ke, . SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF-1-2-(-N-METHYL-N-SUBSTITUTED-BENZYL)AMINO-2-(2,4-DIFLUOROPHENYL) ETHYL-1H-1,2,4-TRIAZOLESJ. Acta Pharmaceutica Sinica, 1999, 34(12): 902-907.
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1-2-(N-甲基-N-取代苄基)氨基-2-(2,4-二氟苯基)乙基-1H-1,2,4-三唑类化合物的合成及抗真菌活性

SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF-1-2-(-N-METHYL-N-SUBSTITUTED-BENZYL)AMINO-2-(2,4-DIFLUOROPHENYL) ETHYL-1H-1,2,4-TRIAZOLES

    摘要
  • 摘要: 目的:1-2-(N-甲基-N-取代苄基)氨基-2-(2,4-二氟苯基) 乙基-1H-1,2 ,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-1H-1 ,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。

     

    Abstract: AIM: To study the synthesis and antifungal activities of 1-2-(Nmethyl-Nsubstituted-benzyl)amino-2-(2,4 difluorophenyl)ethyl-1H-1,2,4-triazoles. METHODS: Key intermediate were prepared by Friedel-Crafts reaction, triazolyl alkylation, ketimine reduction and Leuckart reaction. The title compounds were synthesised by Nalkylation. Antifungal activities in vitro were measured by the two times dilution method. RESULTS: Twentythree 1-2-(Nmethyl-Nsubstituted-benzyl)amino-2-(2,4-difluorophenyl)ethyl-1H-1,2,4-triazoles were synthesised and first reported. All the title compounds exhibited activities against eight fungi. Many of them showed more potent antifungal activities than butenafine against Candida albicans and Candida parapsilosis. The antifungal activities of compounds 1,2,6,13,14 and 19 are 8～32 times more active than econazole against Candida albicans.Compounds 2 and 4 are 4 and 8 times more active than butenafine and 64 and 128 times more than econazole against Cryptococcus neoformans respectively. All the compounds showed equal or more potent activity against Microsporum caniso compared with econazole. CONCLUSION: Some title compounds showed strong antifungal activities and should be studied further.

     

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