Novel semisynthetic vancomycin derivatives with antibacterial activity against vancomycin-resistant S. aureus (VRSA) were prepared. Replacement of Cl groups of vancomycin by Suzuki-Miyaura crosscoupling reaction, which gave the title compounds, is described for the first time. Introduction of a carbon substituent at the amino acid residue 2 of vancomycin led to an enhancement of antibacterial activity against vancomycin-resistant strains, whereas the additional introduction at the amino acid residue 6 resulted in a reduction in activity even against vancomycin-susceptible strains.
|Number of pages||6|
|Journal||Journal of Medicinal Chemistry|
|Publication status||Published - 2010 Mar 25|
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery