Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanol
Yu Zhou, Shichong Yu, Baogang Wang, Yongzheng Yan, WU Qiu-ye
Abstract
Yu Zhou, Shichong Yu, Baogang Wang, Yongzheng Yan, WU Qiu-ye
Abstract
Objective To study the antifungal activity of triazole alcohols by introduction of n-butyl and triazole as side chains.Methods A total of 16 compounds of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanol were synthesized and characterized by 1HNMR and LC-MS.The in vitro antifungal activities of the compounds were determined by tests with 8 human pathogenic fungi.Results It was found that all the 16 title compounds exhibited antifungal activities,and compounds 7b,7d,7e and 7i had antifungal activities stronger than fluconazole,similar to itraconazole.Conclusion Introduction of n-butyl and triazole side chain can confer antifungal activities to the compounds.
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Objective To study the antifungal activity of triazole alcohols by introduction of n-butyl and triazole as side chains.Methods A total of 16 compounds of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanol were synthesized and characterized by 1HNMR and LC-MS.The in vitro antifungal activities of the compounds were determined by tests with 8 human pathogenic fungi.Results It was found that all the 16 title compounds exhibited antifungal activities,and compounds 7b,7d,7e and 7i had antifungal activities stronger than fluconazole,similar to itraconazole.Conclusion Introduction of n-butyl and triazole side chain can confer antifungal activities to the compounds.
Key concepts: Fluconazole, Antifungal, Itraconazole, Triazole, Chemistry, 1,2,4-Triazole, In vitro, Side chain