Lipidated Peptidomimetics with Improved Antimicrobial Activity

We report a series of lipidated alpha-AApeptides that mimic the structure and function of natural antimicrobial lipopeptides. Several short lipidated alpha-AApeptides show broad-spectrum activity against a range of clinically related Gram-positive and Gram-negative bacteria as well as fungus. Their antimicrobial activity and selectivity are comparable or even superior to the clinical candidate pexiganan as well as previously reported linear alpha-AApeptides. The further development of lipidated alpha-AApeptides will lead to a new class of antibiotics to combat drug resistance.