N-alkyl-substituted glycopeptide antibiotics

The glycopeptide antibiotic vancomycin has proved valuable in the treatment of staphylococcal and enterococcal infections, particularly those caused by strains resistant to other antibiotics. The emergence of high-level resistance to vancomycin within the enterococci, and its potential for transfer to other pathogenic Gram-positive cocci, has led to interest in developing new glycopeptide antibiotics with activity against vancomycin resistant organisms. The N-alkylated glycopeptide antibiotics, under development by Lilly Research Laboratories, represent a new series of compounds possessing these properties. The lead compound in this series, LY 333328, is reported to be in Phase I trials.