The First Dimeric Derivatives of the Glycopeptide Antibiotic Teicoplanin

Autor: Ilona Bereczki, Zsolt Szűcs, Gyula Batta, Tamás Milán Nagy, Eszter Ostorházi, Katalin E. Kövér, Anikó Borbás, Pál Herczegh
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Pharmaceuticals, Vol 15, Iss 1, p 77 (2022)
Druh dokumentu: article
ISSN: 1424-8247
DOI: 10.3390/ph15010077
Popis: Various dimeric derivatives of the glycopeptide antibiotic teicoplanin were prepared with the aim of increasing the activity of the parent compound against glycopeptide-resistant bacteria, primarily vancomycin-resistant enterococci. Starting from teicoplanin, four covalent dimers were prepared in two orientations, using an α,ω-bis-isothiocyanate linker. Formation of a dimeric cobalt coordination complex of an N-terminal L-histidyl derivative of teicoplanin pseudoaglycone has been detected and its antibacterial activity evaluated. The Co(III)-induced dimerization of the histidyl derivative was demonstrated by DOSY experiments. Both the covalent and the complex dimeric derivatives showed high activity against VanA teicoplanin-resistant enterococci, but their activity against other tested bacterial strains did not exceed that of the monomeric compounds.
Databáze: Directory of Open Access Journals
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