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Synthesis and Antifungal Activities of 2-(2,4-Difluorophenyl)-3-(N-Methyl-N-Substituted Sulfonamido)-1-(1H-1,2,4-Triazol-1-yl)-2-Propanol

Zhong Wu, Zhang Wannian, Li Ke, Zhou Youjun, Zhu Ju, Lu Jiaguo   

  1. College of Pharmacy, Second Military Medical University, Shanghai 200433
  • Received:1999-03-01 Revised:1999-04-26 Online:2000-03-15 Published:2000-03-15

Abstract: Ten new antifungal triazoles, 3-sulfonamido-2-aryl-1-triazoly-2-propanol derivatives were designed and synthesized as potential inhibitors of the fungal cytochrome P-450 14α-demethylase. Results of antifungal tests in vitro showed that compounds 1b, 1c and 1g had high activity, especially against Candida albicans, Candida parapsilosis and Fonsecaea pedrosor, but less active in comparison with ketoconazole. Compared with fluconazole, compound 1b was thirty-two times more active against Candida parapsilosis and four times more active against Fonsecaea pedrosor, compound 1c was sixteen times more active against Candida parapsilosis and eight times more active against Fonsecaea pedrosor, compound 1g was four times and eight times more active against Candida parapsilosis and Fonsecaea pedrosor respectively.

Key words: Triazoles, Triazoles, Synthesis, Synthesis, Antifungal activity, Antifungal activity

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