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新型半合成替考拉宁衍生物对临床分离的 VRE 的体外活性与奥他万星相当。

New semisynthetic teicoplanin derivatives have comparable in vitro activity to that of oritavancin against clinical isolates of VRE.

机构信息

Department of Pharmaceutical Chemistry, University of Debrecen, Egyetem tér 1, Debrecen, H-4032, Hungary.

Department of Medical Microbiology, Semmelweis University, Nagyvárad tér 4, Budapest, H-1089, Hungary.

出版信息

J Antibiot (Tokyo). 2019 Jul;72(7):524-534. doi: 10.1038/s41429-019-0164-1. Epub 2019 Mar 15.

Abstract

Ten analogues of a teicoplanin pseudoaglycon derivative have been synthesized with the aim of optimizing the in vitro activity of the compound against VanA type vancomycin resistant enterococci (VRE) isolated from hospitalized patients. Teicoplanin, vancomycin, and oritavancin were used as reference antibiotics for the antibacterial evaluations. One of the new derivatives exhibited far superior activity than the original compound. The in vitro MICs measured were comparable to that of oritavancin against the investigated VRE strains.

摘要

已经合成了泰利霉素假糖基衍生物的 10 个类似物,旨在优化该化合物对住院患者分离的 VanA 型万古霉素耐药肠球菌(VRE)的体外活性。替考拉宁、万古霉素和奥他万星被用作抗菌评估的参考抗生素。新衍生物之一的活性远远优于原始化合物。测量的体外 MIC 与奥他万星对所研究的 VRE 菌株的活性相当。

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