Synthesis of paenipeptin C′ analogues employing solution-phase CLipPA chemistry?

Organic & Biomolecular Chemistry Pub Date: 2020-05-26 DOI: 10.1039/D0OB00950D

Abstract

We herein report the synthesis of analogues of the antimicrobial lipopeptide, paenipeptin C′, by installing varying lipid moieties using thiol–ene CLipPA (Cysteine Lipidation on a Peptide or Amino Acid) chemistry. Biological evaluation against both Gram-negative and Gram-positive strains indicated that several analogues possessed potent broad-spectrum antimicrobial activity.

Graphical abstract: Synthesis of paenipeptin C′ analogues employing solution-phase CLipPA chemistry
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