Each year vancomycin resistant <i>Staphylococcus aureus </i>(VRSA) infects 1 million people and kills 11,500. VRSA has caused a growing health concern because the first case was reported in the United States in 2002. Vancomycin was initially used as a last resort treatment for methicillin resistant <i>Staphylococcus aureus</i> (MRSA). As a result, VRSA strains are often resistant to multiple drug classes including beta-lactams and glycopeptide antibiotics. Antibiotic adjuvants may be a promising new approach to combat antibiotic resistance because they potentiate our existing antibiotic arsenal. We screened a library of compounds for the ability to potentiate vancomycin in both VRSA and VISA strains. Novel scaffolds were identified from the active structures and a preliminary structure-activity relationship (SAR) was produced. Biological data, SAR, and initial mechanism of action studies will be presented.

Identification and evaluation of small molecules that potentiate vancomycin in VISA and VRSA

ACS Spring Meeting 2021

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