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Synthesis of Antibacterial Nisin-Peptoid Hybrids Using Click Methodology
Version 1
: Received: 31 May 2018 / Approved: 1 June 2018 / Online: 1 June 2018 (06:18:06 CEST)
A peer-reviewed article of this Preprint also exists.
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. 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.
Abstract
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 µM activity (comparable to natural nisin) against methicillin-resistant Staphylococcus aureus.
Keywords
peptoids; peptoid-peptide hybrid; nisin; antibacterial; alkyne-azide click reactions
Subject
Chemistry and Materials Science, Organic Chemistry
Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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