2007Zhongguo yaowu huaxue zazhiRequires access

Synthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-yl)-2-(t-butyl)-3-(O-substituted)-2-propanols

Zhao Li-hua

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Abstract

Aim To study the antifungal activities of triazole derivatives bearing tert-butyl group and to compare their antifungal activities with that of the control drugs fluconazole and itraconazole.Methods Twelve target compounds were designed by the replacement of 2,4-difluorophenyl group with tert-butyl moiety.The target compounds were confirmed by 1H-NMR and IR.The MIC80 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 and conclusion All the target compounds were firstly reported.The results of the preliminary antifungal test show that all the target compounds exhibit potent antifungal activities to a certain extent.Other hydrophobic moieties besides 2,4-difluorophenyl group can be introduced to design triazole compounds.

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What this paper is about

Aim To study the antifungal activities of triazole derivatives bearing tert-butyl group and to compare their antifungal activities with that of the control drugs fluconazole and itraconazole.Methods Twelve target compounds were designed by the replacement of 2,4-difluorophenyl group with tert-butyl moiety.The target compounds were confirmed by 1H-NMR and IR.The MIC80 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 and conclusion All the target compounds were firstly reported.The results of the preliminary antifungal test show that all the target compounds exhibit potent antifungal activities to a certain extent.Other hydrophobic moieties besides 2,4-difluorophenyl group can be introduced to design triazole compounds.

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Available abstract

Aim To study the antifungal activities of triazole derivatives bearing tert-butyl group and to compare their antifungal activities with that of the control drugs fluconazole and itraconazole.Methods Twelve target compounds were designed by the replacement of 2,4-difluorophenyl group with tert-butyl moiety.The target compounds were confirmed by 1H-NMR and IR.The MIC80 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 and conclusion All the target compounds were firstly reported.The results of the preliminary antifungal test show that all the target compounds exhibit potent antifungal activities to a certain extent.Other hydrophobic moieties besides 2,4-difluorophenyl group can be introduced to design triazole compounds.

Key concepts: Fluconazole, Chemistry, Antifungal, Moiety, Itraconazole, Triazole, Proton NMR, Stereochemistry

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Synthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-yl)-2-(t-butyl)-3-(O-substituted)-2-propanols — Research Paper | ScholarLens