Today, there is a clear need for new antibiotics to treat drug-resistant bacterial infections. Antibiotics that operate by new mechanisms or belong to new structural classes are attractive because they are less likely to show cross-resistance with existing antibiotics. One such antibiotic is ramoplanin which is currently in Phase III clinical trials for the prevention of vancomycin-resistant enterococcal infections in hospitalized patients. Initial results show that the transglycosilation step of peptidoglycan biosynthesis is the likely target for this molecule.