楚勇, 徐鸣夏, 吕丁. 新型三唑类抗真菌化合物的合成及其活性初探J. 药学学报, 2004, 39(11): 904-909.
引用本文: 楚勇, 徐鸣夏, 吕丁. 新型三唑类抗真菌化合物的合成及其活性初探J. 药学学报, 2004, 39(11): 904-909.
CHU Yong, XU Ming-xia, Lü Ding. Synthesis of novel antifungal triazoles and study on their activityJ. Acta Pharmaceutica Sinica, 2004, 39(11): 904-909.
Citation: CHU Yong, XU Ming-xia, Lü Ding. Synthesis of novel antifungal triazoles and study on their activityJ. Acta Pharmaceutica Sinica, 2004, 39(11): 904-909.

新型三唑类抗真菌化合物的合成及其活性初探

Synthesis of novel antifungal triazoles and study on their activity

  • 摘要: 目的设计、合成三唑类抗真菌新化合物并进行活性筛选。方法分别以咪康唑和伊曲康唑为先导化合物,根据相关构效关系进行设计并合成;采用纸片琼脂扩散法和96孔微量稀释法测定各新化合物的体外抑菌活性。结果合成了12个1-三唑基-2-氟代苯基-3-取代氨基-2-丙醇类新化合物(M)和13个2-取代苯基-5-三唑甲基-5-氟代苯基-N-取代恶唑烷类新化合物(A),用MS,1HNMR确证结构。大多数目标化合物对白色念珠菌有一定抑制活性,其中A10,A12,A13的活性强于对照品氟康唑和伊曲康唑,且对酵母菌亦显示一定抑制作用。结论化合物A10,A12,A13值得进一步研究。

     

    Abstract: AimDesign, synthesis and activity study of novel antifungal triazoles. MethodsThe 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. ResultsTwelve 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. ConclusionCompounds A10, A12 and A13 are worthy to be intensively studied.

     

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