Design and synthesis of membrane-targeting antibiotics: from peptides- to aminosugar-based antimicrobial cationic amphiphiles

Infections caused by drug resistant and/or slow-growing bacteria are increasingly becoming some of the greatest challenges of health organizations worldwide. The decrease in the efficacy of a large percentage of the current repertoire of clinically used antibiotics against these types of infections emphasizes the need for the development of novel antimicrobial agents that will effectively eradicate a broad spectrum of bacteria regardless of the bacterial cell cycle stage. In this Review, we present recent years' progress in the development of cationic amphiphiles that target the bacterial membrane bilayer as a strategy for the development of antibiotics. Synthesis, antimicrobial activity, membrane selectivity and modes of action aspects are discussed.