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Synthesis of Antibacterial Nisin?Peptoid Hybrids Using Click Methodology.

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 micromolar activity (comparable to natural nisin) against methicillin-resistant Staphylococcus aureus.

SUBMITTER: Bolt HL

PROVIDER: S-EPMC6099617 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature

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Synthesis of Antibacterial Nisin⁻Peptoid Hybrids Using Click Methodology.

Bolt Hannah L HL Kleijn Laurens H J LHJ Martin Nathaniel I NI Cobb Steven L SL

Molecules (Basel, Switzerland) 20180628 7

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 ...[more]

PMID: 29958423

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