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 have been prepared with free and amide C-terminal parts. Six aliphatic and aromatic lipophilic carbodiimides were prepared and used for the synthesis of lipophilic guanidine teicoplanin conjugates. All new N-terminal guanidine antibiotics showed high activity against a standard panel of Gram-positive bacteria. Four selected derivatives displayed excellent antibacterial activity against a series of nosocomial VanA Enterococcus faecium strains.

中文翻译：

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替考拉宁抗生素的N末端胍衍生物对糖肽抵抗性粪肠球菌具有强活性。

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。