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Development of truncated Battacin antimicrobials featuring novel N-terminal fatty acids with an excellent safety profile.

Authors
  • Posa, Luka1
  • Tomek, Petr2
  • Lamba, Saurabh1
  • Sarojini, Vijayalekshmi3
  • Barker, David4
  • 1 School of Chemical Sciences, University of Auckland, Auckland, New Zealand. , (New Zealand)
  • 2 Auckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, School of Medical Sciences, University of Auckland, 85 Park Road, Grafton, Auckland 1023, New Zealand. , (New Zealand)
  • 3 School of Chemical Sciences, University of Auckland, Auckland, New Zealand; Macdiarmid Institute for Advanced Materials and Nanotechnology, Wellington 6012, New Zealand. Electronic address: [email protected]. , (New Zealand)
  • 4 School of Chemical Sciences, University of Auckland, Auckland, New Zealand; Macdiarmid Institute for Advanced Materials and Nanotechnology, Wellington 6012, New Zealand. Electronic address: [email protected]. , (New Zealand)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Nov 15, 2023
Volume
96
Pages
129535–129535
Identifiers
DOI: 10.1016/j.bmcl.2023.129535
PMID: 37871890
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

Octapeptin B5 peptides containing a novel fatty acids have been found to have enhanced antibacterial activity against Staphylococcus aureus and also have an excellent safety profile. Cyclic lipopeptides such as the polymyxins and battacin are potent antibacterial agents. It has been shown that truncated, non-linear, versions of these agents (e.g. octapeptin B5) can retain the activity of the more complex cyclic compounds. In this work the synthesis of Octapeptin B5 peptides containing a range of novel fatty acids is reported. Many of these lipopeptides have been found to have enhanced antibacterial activity against Staphylococcus aureus compared to Octapeptin B5 whilst also having an excellent safety profile in haemolytic and cytotoxicity assays. Copyright © 2023 The Author(s). Published by Elsevier Ltd.. All rights reserved.

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