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Keywords:

  • aminoglycoside-modifying enzymes;
  • amphiphiles;
  • antibiotics;
  • glycosides;
  • hemolysis
Thumbnail image of graphical abstract

Amphiphilic aminoglycoside antibiotics kill bacteria by disruption of their highly negatively charged membrane. In their Communication on page 5652 ff., M. Fridman, S. Garneau-Tsodikova, and co-workers report the synthesis of 6′′-thioether tobramycin derivatives and show that their aliphatic chain acts as a drill bit that can rupture bacterial cells. These potent compounds evade many of the common bacterial resistance mechanisms, thereby opening a new avenue for the discovery of membrane-targeting antibiotics.