N-Terminal guanidine derivatives of teicoplanin antibiotics strongly active against glycopeptide resistant Enterococcus faecium

Zsolt Szűcs, Ilona Bereczki, Erzsébet Rőth, Márton Milánkovits, Eszter Ostorházi, Gyula Batta, Lajos Nagy, Zsuzsanna Dombrádi, Anikó Borbás, Pál Herczegh

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish
JournalJournal of Antibiotics
DOIs
Publication statusAccepted/In press - Jan 1 2020

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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    Szűcs, Z., Bereczki, I., Rőth, E., Milánkovits, M., Ostorházi, E., Batta, G., Nagy, L., Dombrádi, Z., Borbás, A., & Herczegh, P. (Accepted/In press). N-Terminal guanidine derivatives of teicoplanin antibiotics strongly active against glycopeptide resistant Enterococcus faecium. Journal of Antibiotics. https://doi.org/10.1038/s41429-020-0313-6