Synthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols
Wan Zhang
Abstract
Wan Zhang
Abstract
Objective: Eight new fluconazole derivatives 1 (1H 1,2,4 triazol 1 yl) 2 (2,4 difluorophenyl)3 substituted 2 propanols were designed and synthesized in search for more potent, less toxic and broad spectrum antimycotics. Methods: All the compounds were synthesized and confirmed by elementary analysis, 1HNMR and IR spectra. The antifungal activities of the compounds were evaluated in vitro by Sabourand′s method. Results: The results of preliminary antifungal test showed that all of the compounds were of high activities against 7 common pathogenic fungi. Conclusion: Compounds Ⅷ 1,Ⅷ 4, Ⅷ 5, Ⅷ 8 have excellent antifungal activities and have potential prospect to be further developed.
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Objective: Eight new fluconazole derivatives 1 (1H 1,2,4 triazol 1 yl) 2 (2,4 difluorophenyl)3 substituted 2 propanols were designed and synthesized in search for more potent, less toxic and broad spectrum antimycotics. Methods: All the compounds were synthesized and confirmed by elementary analysis, 1HNMR and IR spectra. The antifungal activities of the compounds were evaluated in vitro by Sabourand′s method. Results: The results of preliminary antifungal test showed that all of the compounds were of high activities against 7 common pathogenic fungi. Conclusion: Compounds Ⅷ 1,Ⅷ 4, Ⅷ 5, Ⅷ 8 have excellent antifungal activities and have potential prospect to be further developed.
Key concepts: Antifungal, Fluconazole, Broad spectrum, Chemistry, In vitro, Combinatorial chemistry, Stereochemistry, Microbiology