| N-〔3-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-2-羟基-丙基〕-氨基乙酸及其衍生物的合成和抗真菌活性 |
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| 引用本文： | 徐俊,周廷森,刘超美,吴义杰,张大志. N-〔3-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-2-羟基-丙基〕-氨基乙酸及其衍生物的合成和抗真菌活性[J]. 中国药物化学杂志, 1998, 0(3) |
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| 作者姓名： | 徐俊 周廷森 刘超美 吴义杰 张大志 |
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| 作者单位： | 第二军医大学药学院 |
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| 摘 要： | 设计合成了Ｎ〔３（１Ｈ１，２，４三唑１基）２（２，４二氟苯基）２羟基丙基〕氨基乙酸及其９个衍生物，均为未见文献报道的新化合物，初步药理试验表明：部分化合物对浅部真菌有一定的活性，除卡氏枝孢霉菌外，对其它深部真菌活性较弱，其中化合物（５ｅ），（５ｈ）对某些真菌的体外活性较强，明显优于氟康唑，但稍弱于酮康唑
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| 关 键 词： | 三唑氨基醇；抗真菌活性；合成；构效关系 |
Synthesis and Antifungal Activity of N-3-(1- H -1,2,4-Triazole-1-yl)-2- (2,4-Difluorophenyl)-2-Hydroxyl-Propyl-Aminoacetic Acid and Its Derivatives |
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| Xu Jun,Zhou Tingsen,Liu Chaomei,Wu Yijie,Zhang Dazhi. Synthesis and Antifungal Activity of N-3-(1- H -1,2,4-Triazole-1-yl)-2- (2,4-Difluorophenyl)-2-Hydroxyl-Propyl-Aminoacetic Acid and Its Derivatives[J]. Chinese Journal of Medicinal Chemistry, 1998, 0(3) |
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| Authors: | Xu Jun Zhou Tingsen Liu Chaomei Wu Yijie Zhang Dazhi |
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| Abstract: | N-3-(1- H -1,2,4-Triazole-1-yl)-2- (2,4-Difluorophenyl)-2-Hydroxyl-Propyl-Aminoacetic Acid and its nine derivatives were designed and synthesized and evaluated for antifungal activities in vitro .The synthetic methods of the title compounds and the intermediates have not been reported in literature and all of the compounds are first reported.The results of preliminary antifungal tests showed that some compounds exhibited potent activities against dermophytes ,but lower activities against systematic pathogenic fungi except cladosporium carioni .Compared with fluconazole,the activities of compounds (5e) and (5h) were markedly superior,but were less potent than those of ketoconazole in vitro . |
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| Keywords: | triazole amino alcohol antifungal activity synthesis structure activity relationship |
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