Synthesis of Antibacterial Nisin–Peptoid Hybrids Using Click Methodology
1
Center for Global Infectious Diseases, Department of Chemistry, Durham University, South Road, Durham DH1 3LE, UK
2
Department of Medicinal Chemistry and Chemical Biology, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, Universiteitsweg 99, 3584 CG Utrecht, The Netherlands
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Molecules 2018, 23(7), 1566; https://doi.org/10.3390/molecules23071566
Received: 31 May 2018 / Revised: 18 June 2018 / Accepted: 21 June 2018 / Published: 28 June 2018
(This article belongs to the Special Issue Antimicrobial Peptides and Peptidomimetics)
Antimicrobial peptides and structurally related peptoids offer potential for the development of new antibiotics. However, progress has been hindered by challenges presented by poor in vivo stability (peptides) or lack of selectivity (peptoids). Herein, we have developed a process to prepare novel hybrid antibacterial agents that combine both linear peptoids (increased in vivo stability compared to peptides) and a nisin fragment (lipid II targeting domain). The hybrid nisin–peptoids prepared were shown to have low micromolar activity (comparable to natural nisin) against methicillin-resistant Staphylococcus aureus.
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MDPI and ACS Style
Bolt, H.L.; Kleijn, L.H.J.; Martin, N.I.; Cobb, S.L. Synthesis of Antibacterial Nisin–Peptoid Hybrids Using Click Methodology. Molecules 2018, 23, 1566.
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