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: |
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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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