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Recent advances in synthetic lipopeptides as anti-microbial agents: designs and synthetic approaches

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Abstract

Infectious diseases impose serious public health burdens and continue to be a global public health crisis. The treatment of infections caused by multidrug-resistant pathogens is challenging because only a few viable therapeutic options are clinically available. The emergence and risk of drug-resistant superbugs and the dearth of new classes of antibiotics have drawn increasing awareness that we may return to the pre-antibiotic era. To date, lipopeptides have been received considerable attention because of the following properties: They exhibit potent antimicrobial activities against a broad spectrum of pathogens, rapid bactericidal activity and have a different antimicrobial action compared with most of the conventional antibiotics used today and very slow development of drug resistance tendency. In general, lipopeptides can be structurally classified into two parts: a hydrophilic peptide moiety and a hydrophobic fatty acyl chain. To date, a significant amount of design and synthesis of lipopeptides have been done to improve the therapeutic potential of lipopeptides. This review will present the current knowledge and the recent research in design and synthesis of new lipopeptides and their derivatives in the last 5 years.

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Acknowledgements

This work was supported by the Singhealth foundation research grant (SHF/FG691S/2016), National Medical Research Council (NMRC/CBRG/0080/2015 and NMRC/TCR/R1018) and the Singhealth Foundation (SHF/FG538P/2013).

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Authors and Affiliations

  1. Singapore Eye Research Institute, The Academia, 20 College Road, Discovery Tower Level 6, Singapore, 169856, Singapore

    Jun-Jie Koh, Shuimu Lin, Roger W. Beuerman & Shouping Liu

  2. School of Materials Science and Engineering, South China University of Technology, Guangzhou, 510641, China

    Shuimu Lin

  3. SRP Neuroscience and Behavioral Disorders, Duke-NUS Medical School, Singapore, 169857, Singapore

    Roger W. Beuerman & Shouping Liu

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  1. Jun-Jie Koh
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  2. Shuimu Lin
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Koh, JJ., Lin, S., Beuerman, R.W. et al. Recent advances in synthetic lipopeptides as anti-microbial agents: designs and synthetic approaches. Amino Acids 49, 1653–1677 (2017). https://doi.org/10.1007/s00726-017-2476-4

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