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Issue 8, 2012
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Design and synthesis of unprecedented cyclic γ-AApeptides for antimicrobial development

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Abstract

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 γ-AApeptides via an on-resin cyclization. These cyclic γ-AApeptides are potent and broad-spectrum active against fungus and multi-drug resistant Gram-positive and Gram-negative bacterial pathogens. Our results demonstrate the potential of cyclic γ-AApeptides as a new class of antibiotics to circumvent drug resistance by mimicking the bactericidal mechanism of AMPs. Meanwhile, the facile synthesis of cyclic γ-AApeptides may further expand the applications of γ-AApeptides in biomedical sciences.

Graphical abstract: Design and synthesis of unprecedented cyclic γ-AApeptides for antimicrobial development

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Publication details

The article was received on 05 Apr 2012, accepted on 17 May 2012 and first published on 17 May 2012


Article type: Edge Article
DOI: 10.1039/C2SC20428B
Citation: Chem. Sci., 2012,3, 2570-2575
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    Design and synthesis of unprecedented cyclic γ-AApeptides for antimicrobial development

    H. Wu, Y. Niu, S. Padhee, R. E. Wang, Y. Li, Q. Qiao, G. Bai, C. Cao and J. Cai, Chem. Sci., 2012, 3, 2570
    DOI: 10.1039/C2SC20428B

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