N-Terminal guanidine derivatives of teicoplanin antibiotics strongly active against glycopeptide resistant Enterococcus faecium
作者:Zsolt Szűcs、Ilona Bereczki、Erzsébet Rőth、Márton Milánkovits、Eszter Ostorházi、Gyula Batta、Lajos Nagy、Zsuzsanna Dombrádi、Anikó Borbás、Pál Herczegh
DOI:10.1038/s41429-020-0313-6
日期:2020.9
Antibiotic resistance is one of the major challenges in healthcare of our time. To meet this challenge, we designed and prepared guanidine and lipophilic guanidine derivatives of the glycopeptide antibiotic teicoplanin to armed them with activity against the most threatening nosocomial bacteria, multiresistant enterococci. From teicoplanin and its pseudoaglycone, a series of N-terminal guanidine derivatives
抗生素耐药性是当今时代医疗保健的主要挑战之一。为了应对这一挑战,我们设计并制备了糖肽抗生素替考拉宁的胍和亲脂胍衍生物,使其具有抵抗最具威胁性的医院细菌多耐药肠球菌的活性。由替考拉宁及其假糖苷配基制备了具有游离和酰胺C端部分的一系列N端胍衍生物。制备了六个脂族和芳族亲脂性碳二亚胺,并用于合成亲脂性胍替考拉宁缀合物。所有新的N末端胍类抗生素均对标准的革兰氏阳性菌显示出高活性。四个选定的衍生物显示出对一系列院内VanA肠球菌粪便菌株的优异抗菌活性。