AI Article Synopsis
- Researchers modified teicoplanin, a glycopeptide antibiotic, by creating various dimeric forms to enhance its effectiveness against glycopeptide-resistant bacteria, especially vancomycin-resistant enterococci.
- Four covalent dimers were synthesized using a specific linker and an experiment detected a dimeric complex involving a histidyl version of teicoplanin.
- The created dimeric derivatives were found to be very effective against the resistant enterococci, although their effectiveness against other bacterial strains was similar to that of the original, non-dimerized teicoplanin.
Article Abstract
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 -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.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8779952 | PMC |
| http://dx.doi.org/10.3390/ph15010077 | DOI Listing |
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