Synthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted)-piperazin-1-yl]-2-propanols
Yongbing Cao
Abstract
Yongbing Cao
Abstract
Aim To design and synthesis triazole derivatives with the side chain containing 4-substitued-piperazin-1-yl and to investigate their antifungal activities in vitro.Methods According to the structure of fluconazole,eleven target compounds were designed and synthesized.All of them were confirmed by()1H-NMR or IR spectra,respectively.The MIC(80) of all the target compounds were determined by the method recommended by the national committee for clinical laboratory standards(NCCLS) using the RPMI 1640 test medium.Results Eleven target compounds were firstly reported.The results of the preliminary antifungal test showed that all the target compounds exhibited potent antifungal activities to a certain extent.Conclusion Most of the target compounds showed higher antifungal activities than that of fluconazole.Especially,compound 11 showed strong antifungal activity with broad antifungal spectrum and is chosen for further study.
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Aim To design and synthesis triazole derivatives with the side chain containing 4-substitued-piperazin-1-yl and to investigate their antifungal activities in vitro.Methods According to the structure of fluconazole,eleven target compounds were designed and synthesized.All of them were confirmed by()1H-NMR or IR spectra,respectively.The MIC(80) of all the target compounds were determined by the method recommended by the national committee for clinical laboratory standards(NCCLS) using the RPMI 1640 test medium.Results Eleven target compounds were firstly reported.The results of the preliminary antifungal test showed that all the target compounds exhibited potent antifungal activities to a certain extent.Conclusion Most of the target compounds showed higher antifungal activities than that of fluconazole.Especially,compound 11 showed strong antifungal activity with broad antifungal spectrum and is chosen for further study.
Key concepts: Fluconazole, Antifungal, Chemistry, Triazole, In vitro, Proton NMR, Broad spectrum, Stereochemistry