Lipopeptidomimetics derived from teixobactin have potent antibacterial activity against Staphylococcus aureus.
Georgina C GirtAmit MahindraZaaima J H Al JabriMegan De Ste CroixMarco R OggioniAndrew G JamiesonPublished in: Chemical communications (Cambridge, England) (2018)
A series of lipopeptidomimetics derived from teixobactin have been prepared that probe the role of residues (1-6) as a membrane anchor and the function of enduracididine. The most active compounds, with a farnesyl tail and End10 to Lys10 or Orn10 substitution have potent activity (MIC 8 μg mL-1) against S. aureus. These results pave the way for the synthesis of simple, cost-effective yet potent lipopeptidomimetic antimicrobials.