Synthesis and biological evaluation of lipophilic teicoplanin pseudoaglycon derivatives containing a substituted triazole function

Szucs Zsolt; Csavas Magdolna; Roth Erzsebet; Borbas Aniko; Batta Gyula; Perret Florent; Ostorhazi Eszter; Szatmari Reka; Vanderlinden Evelien; Naesens Lieve; Herczegh Pal

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Synthesis and biological evaluation of lipophilic teicoplanin pseudoaglycon derivatives containing a substituted triazole function

机译：含有取代三唑函数的亲脂性Teicoplanin的合成与生物学评价

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A series of lipophilic teicoplanin pseudoaglycon derivatives, including alkyl-, aryl-, calixarene-and protected sugar-containing conjugates, were prepared using azide-alkyne click chemistry. Out of the conditions applied, the CuSO4-ascorbate reagent system proved to be more efficient than the Cu(I)I-Et3N-mediated reaction. Some of the new compounds have high in vitro activity against glycopeptide-resistant Gram-positive bacteria, including vanA-positive Enterococcus faecalis. A few of them also display promising in vitro anti-influenza activity.

机译：使用叠氮化物 - 烷烃咔哒化学制备了一系列亲脂性Teicoplanin伪蛋白衍生物，包括烷基，芳基 - ，钙芳烃和保护的含糖缀合物。出于所施加的条件下，CusO4抗坏血酸试剂系统被证明比Cu（I）I-ET3N介导的反应更有效。一些新化合物对抗糖肽抗革兰氏阳性细菌具有高的体外活性，包括Vana阳性肠球菌粪便。其中一些也展示了有前途的体外抗流感活动。

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《The Journal of Antibiotics: An International Journal》 |2017年第2期|共6页
作者
Szucs Zsolt; Csavas Magdolna; Roth Erzsebet; Borbas Aniko; Batta Gyula; Perret Florent; Ostorhazi Eszter; Szatmari Reka; Vanderlinden Evelien; Naesens Lieve; Herczegh Pal;
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Univ Debrecen Dept Pharmaceut Chem Egyet Ter 1 H-4010 Debrecen Hungary;

Univ Debrecen Dept Pharmaceut Chem Egyet Ter 1 H-4010 Debrecen Hungary;

Univ Debrecen Dept Pharmaceut Chem Egyet Ter 1 H-4010 Debrecen Hungary;

Univ Debrecen Dept Pharmaceut Chem Egyet Ter 1 H-4010 Debrecen Hungary;

Univ Debrecen Dept Organ Chem Debrecen Hungary;

Univ Lyon 1 ICBMS Equipe CSAp Villeurbanne France;

Semmelweis Univ Dept Med Microbiol Budapest Hungary;

Semmelweis Univ Dept Med Microbiol Budapest Hungary;

Katholieke Univ Leuven Rega Inst Med Res Leuven Belgium;

Katholieke Univ Leuven Rega Inst Med Res Leuven Belgium;

Univ Debrecen Dept Pharmaceut Chem Egyet Ter 1 H-4010 Debrecen Hungary;

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正文语种 eng
中图分类药学;
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机译：含有取代三唑函数的亲脂性Teicoplanin的合成与生物学评价
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Synthesis and biological evaluation of lipophilic teicoplanin pseudoaglycon derivatives containing a substituted triazole function

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