Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

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

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