Abstract
A series of lipopeptidomimetics derived from teixobactin have been prepared that probe the role of residues (1-6) as a membrane anchor and the function of enduracididine. The most active compounds, with a farnesyl tail and End10 to Lys10 or Orn10 substitution have potent activity (MIC 8 μg mL-1) against S. aureus. These results pave the way for the synthesis of simple, cost-effective yet potent lipopeptidomimetic antimicrobials.
MeSH terms
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Depsipeptides / chemical synthesis
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Depsipeptides / chemistry
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Depsipeptides / pharmacology*
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Dose-Response Relationship, Drug
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Microbial Sensitivity Tests
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Molecular Conformation
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Peptidomimetics*
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Staphylococcus aureus / drug effects*
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Depsipeptides
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Peptidomimetics
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teixobactin