Szűcs Zsolt, Csávás Magdolna, Rőth Erzsébet, Borbás Anikó, Batta Gyula, Perret Florent, Ostorházi Eszter, Szatmári Réka, Vanderlinden Evelien, Naesens Lieve, Herczegh Pál
Department of Pharmaceutical Chemistry, University of Debrecen, Debrecen, Hungary.
Department of Organic Chemistry, University of Debrecen, Debrecen, Hungary.
J Antibiot (Tokyo). 2017 Feb;70(2):152-157. doi: 10.1038/ja.2016.80. Epub 2016 Jun 29.
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 CuSO-ascorbate reagent system proved to be more efficient than the Cu(I)I-EtN-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.
使用叠氮化物-炔烃点击化学制备了一系列亲脂性替考拉宁假糖苷配基衍生物，包括含烷基、芳基、杯芳烃和保护糖的共轭物。在所应用的条件中，硫酸铜-抗坏血酸盐试剂体系被证明比碘化亚铜-乙腈介导的反应更有效。一些新化合物对耐糖肽革兰氏阳性菌具有高体外活性，包括vanA阳性粪肠球菌。其中一些还显示出有前景的体外抗流感活性。
