Development of second generation vancomycin-based antibiotics.

In the last few decades, the tremendous increase in resistance against antibiotics has become a main threat to public health. Methicillin-resistant Staphylococcus aureus (MRSA) is one of the most infamous among all resistant pathogens and vancomycin – a glycopeptide – became the drug of choice (“drug of last resort”) for treating most MRSA infections. However, due to its frequent use, bacteria such as VRSA and VRE have become resistant to it. Millions of dollars are spent each year by healthcare systems trying to control antibiotic-resistant bacteria. We recently developed novel vancomycin-analogs exhibiting promising results against several VRE strains of VanA phenotype and VRSA, while their synthesis is more cost-efficient than competing vancomycin-analogs under development. In the present project, we will optimize the vancomycin-analogs for improved activity and lower cytotoxicity to strengthen our current priority patent applications.