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Vancomycin is a glycopeptide antibiotic that inhibits transpeptidation during cell wall synthesis by binding to the  D -Ala- D -Ala termini of lipid II. For long, it has been used as a last resort antibiotic. However, since the emergence of the first vancomycin-resistant enterococci in 1987, vancomycin resistance has become widespread, especially in hospitals. We have synthesized and evaluated 110 vancomycin analogs modified at the C-terminal carboxyl group of the heptapeptide moiety with R 2 NHR 1 NH 2  substituents. Through iterative optimizations of the substituents, we identified vancomycin analogs that fully restore (or even exceed) the original inhibitory activity against vancomycin-resistant enterococci (VRE), vancomycin-intermediate (VISA) and vancomycin-resistant  Staphylococcus aureus  (VRSA) strains. The best analogs have improved growth inhibitory activity and  in vitro  therapeutic indices against a broad set of VRE and methicillin-resistant  S. aureus  (MRSA) isolates. They also exceed the activity of vancomycin against  Clostridium difficile  ribotypes. Vanc-39 and Vanc-42 have a low probability to provoke antibiotic resistance, and overcome different vancomycin resistance mechanisms (VanA, VanB, and VanC1).

Iterative Chemical Engineering of Vancomycin Leads to Novel Vancomycin Analogs With a High in Vitro Therapeutic Index