Abstract
The increasing incidence of vancomycin resistance in clinical settings has prompted research into new antibiotics against vancomycin–resistant strains. Recent efforts toward the development of novel glycopeptide antibiotics including our works are reviewed. Introduction of a carbon substituent at the amino acid residue 2 of vancomycin by Suzuki–Miyaura cross–coupling reaction led to an enhancement of antibacterial activity against vancomycin–resistant Staphylococcus aureus (VRSA). The potent activities of Van–M–02 against the Gram–positive bacteria including vancomycin–resistant enterococci (VRE) and VRSA are also described, and its mode of action was investigated with an assay system employing cell–membrane fraction of S.aureus as a crude enzyme mixture.
