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  3. Synthetic studies with the brevicidine and laterocidine lipopeptide antibiotics including analogues with enhanced properties and in vivo efficacy

Synthetic studies with the brevicidine and laterocidine lipopeptide antibiotics including analogues with enhanced properties and in vivo efficacy

  • Chem Sci. 2022 Feb 23;13(12):3563-3570. doi: 10.1039/d2sc00143h.
Karol Al Ayed 1,  Ross D Ballantine 2,  Michael Hoekstra 1,  Samantha J Bann 2,  Charlotte M J Wesseling 1,  Alexander T Bakker 3,  Zheng Zhong 4,  Yong-Xin Li 4,  Nora C Brüchle 1,  Mario van der Stelt 3,  Stephen A Cochrane 2,  Nathaniel I Martin 1
Affiliations

Affiliations

  • 1 Biological Chemistry Group, Institute of Biology, Leiden University Sylviusweg 72 2333 BE Leiden The Netherlands n.i.martin@biology.leidenuniv.nl.
  • 2 School of Chemistry and Chemical Engineering, Queen's University Belfast David Keir Building, Stranmillis Road BT9 5AG Belfast UK s.cochrane@qub.ac.uk.
  • 3 Molecular Physiology Group, Leiden Institute of Chemistry, Leiden University Einsteinweg 55 2333 CC Leiden The Netherlands.
  • 4 Department of Chemistry, The University of Hong Kong Pokfulam Road Hong Kong China.
PMID: 35432860 DOI: 10.1039/d2sc00143h
Abstract

Brevicidine and laterocidine are two recently discovered lipopeptide Antibiotics with promising Antibacterial activity. Possessing a macrocyclic core, multiple positive charges, and a lipidated N-terminus, these lipopeptides exhibit potent and selective activity against Gram-negative pathogens, including polymyxin-resistant isolates. Given the low amounts of brevicidine and laterocidine accessible by fermentation of the producing Microorganisms, synthetic routes to these lipopeptides present an attractive alternative. We here report the convenient solid-phase syntheses of both brevicidine and laterocidine and confirm their potent anti-Gram-negative activities. The synthetic routes developed also provide convenient access to novel structural analogues of both brevicidine and laterocidine that display improved hydrolytic stability while maintaining potent Antibacterial activity in both in vitro assays and in vivo Infection models.

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