Yao xue xue bao = Acta pharmaceutica Sinica · 2004
[Synthesis of novel antifungal triazoles and study on their activity].
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Chu Yong, Xu Ming-Xia, Lü Ding
Аннотация
AIM: Design, synthesis and activity study of novel antifungal triazoles.
METHODS: The structures of two lead-compounds miconazole and itrconazole were modified on the basis of SAR studied by our group and reported in the literature and their antifungal activities in vitro were tested by standard program.
RESULTS: Twelve 1-(1H-1, 2, 4-triazole-1-yl) -2-( 2, 4-difluorophenyl)-3-substituted amino-2-propanol compounds and thirteen 2-substituted phenyl-5-(1H-1, 2, 4-triazole-1-methyl ) 5-( 2, 4-difluorophenyl)-N-substituted oxazolidine compounds were synthesized and confirmed by 1HNMR and MS. In vitro inhibitory tests showed that most of them have more or less inhibitory effects on C. albicans and some inhibit S. cerevisiae also. Especially the effects of A10, A12 and A13 on C. albicans were more potent than (or equal to) that of fluconazole or itraconazole.
CONCLUSION: Compounds A10, A12 and A13 are worthy to be intensively studied.
METHODS: The structures of two lead-compounds miconazole and itrconazole were modified on the basis of SAR studied by our group and reported in the literature and their antifungal activities in vitro were tested by standard program.
RESULTS: Twelve 1-(1H-1, 2, 4-triazole-1-yl) -2-( 2, 4-difluorophenyl)-3-substituted amino-2-propanol compounds and thirteen 2-substituted phenyl-5-(1H-1, 2, 4-triazole-1-methyl ) 5-( 2, 4-difluorophenyl)-N-substituted oxazolidine compounds were synthesized and confirmed by 1HNMR and MS. In vitro inhibitory tests showed that most of them have more or less inhibitory effects on C. albicans and some inhibit S. cerevisiae also. Especially the effects of A10, A12 and A13 on C. albicans were more potent than (or equal to) that of fluconazole or itraconazole.
CONCLUSION: Compounds A10, A12 and A13 are worthy to be intensively studied.