Synthesis and antifungal activity of triazole derivatives with side chain containing tert-butyl and 4-substituted piperazin-1-yl / 第二军医大学学报

ABSTRACT

Objective: To design and synthesize the triazole derivatives with the side chain containing tert-butyl and 4-substitued-piperazin-1-yl and to investigate their antifungal activities in vitro. Methods: The triazole derivatives were synthesized through several steps using 3, 3-dimethylbutyryl chloride as the starting material. All the target compounds were confirmed by 1HNMR to be 1-(1H-1, 2, 4-triazol-l-yl)-2-(3, 3-dimethyl)-3-[(4-substituted)-piperazin-l-yl]-2-propanols. Candida albicans (ATCC76615), Cryptococcus neoformans (ATCC32609), Candida tropicalis, Candida parapsilosis, Trichophyton rubrum, Microsporum lauosum, Fonsecaea compacta, and Aspergillus fumigatus were used to test the antifungal activities of the target compounds in vitro according to the National Committee for Clinical Laboratory Standards (NCCLS). Results: Eleven target compounds were obtained and all of them were firstly reported. We also found that all the 11 compounds had certain antifungal activities against the 8 tested strains. Conclusion: Compound 9 has a better effect against Cryptococcus neoformans than fluconazole and itraconazole; compound 8 has a better effect against Aspergillus fumigatus than fluconazole; these two compounds deserve further study.