Journal
CHEMICAL SCIENCE
Volume 3, Issue 8, Pages 2570-2575Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2sc20428b
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- USF Start-up fund
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Antimicrobial drug resistance is one of the greatest threats facing mankind. Antimicrobial peptides (AMPs) can potentially circumvent drug resistance, probably through a bacterial membrane-disruption mechanism. However, they suffer from low in vivo stability, potential immunogenicity, and difficulty in optimization. The development of antimicrobial peptidomimetics is therefore an emerging research area as they avoid the potential disadvantages of AMPs. Cyclic peptidomimetics are of significant interest since constraints induced by cyclization are expected to further improve their antimicrobial activity. Nonetheless, the report of cyclic oligomeric peptidomimetics for antimicrobial development is rare. Herein, for the first time, we report the design and synthesis of cyclic gamma-AApeptides via an on-resin cyclization. These cyclic gamma-AApeptides are potent and broad-spectrum active against fungus and multidrug resistant Gram-positive and Gram-negative bacterial pathogens. Our results demonstrate the potential of cyclic gamma-AApeptides as a new class of antibiotics to circumvent drug resistance by mimicking the bactericidal mechanism of AMPs. Meanwhile, the facile synthesis of cyclic gamma-AApeptides may further expand the applications of gamma-AApeptides in biomedical sciences.
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