Antimicrobials articles within Nature Chemistry

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  • Article |

    Polyether ionophores are natural products that display antibacterial activity—but they also show activity against mammalian cells, which has limited their development as clinical antibiotics. Now, a semisynthesis principle of recycling substructures from highly abundant natural polyether ionophores has been used to prepare analogues with enhanced selectivity towards bacterial cells.

    • Shaoquan Lin
    • , Han Liu
    •  & Thomas B. Poulsen

  • Article |

    Enacyloxin IIa is an antibiotic, assembled by a modular polyketide synthase, with promising activity against the Gram-negative bacterium Acinetobacter baumannii. Now, it has been shown that the enacyloxin IIa polyketide chain is released via transfer to a separately encoded carrier protein by a non-elongating ketosynthase domain, followed by condensation with 3,4-dihydroxycyclohexane carboxylic acid by a non-ribosomal peptide synthetase condensation domain.

    • Joleen Masschelein
    • , Paulina K. Sydor
    •  & Gregory L. Challis

  • Article |

    Bacteria communicate through excretion of minute amounts of chemical signalling molecules that affect virulence, biofilm formation and colonization. In staphylococci, these molecules, called autoinducing peptides, are macrocyclic thiolactone-containing peptides. Now, a simple enrichment method, based on chemoselective capture on polymer beads, has been developed that enables the identification of previously unknown autoinducing peptides.

    • Bengt H. Gless
    • , Martin S. Bojer
    •  & Christian A. Olsen

  • Article |

    Selective modifications of structurally complex molecules bearing multiple reactive functional groups often require cumbersome multistep synthetic efforts. Here, aptameric protective groups based on short RNA sequences are described — they bind to neamine antibiotics, simultaneously protecting several functionalities and enabling regio- and chemoselective functionalizations.

    • Andreas A. Bastian
    • , Alessio Marcozzi
    •  & Andreas Herrmann

  • Article |

    Marinomycin A is a member of a new class of bis-salicylate-containing polyene macrodiolide, with potent antibiotic activity against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VREF). Here, a triply convergent synthesis of this agent is described that uses the salicylate moiety as a novel molecular switch for the chemoselective construction of the macrodiolide.

    • P. Andrew Evans
    • , Mu-Hua Huang
    •  & Sergio Maroto

  • News & Views |

    The tunicamycins, secondary metabolites of various Streptomyces species, are invaluable tools in glycobiology. It has now been shown that their biosynthesis involves an unusual exo-glycal intermediate produced by previously unknown short-chain dehydrogenase/reductase activity.

    • Ethan D. Goddard-Borger
    •  & Stephen G. Withers

  • Article |

    Construction of the remarkable 11-carbon frame of the antibiotic tunicamycin is shown to use cyclic enol ethers (exo-glycals) — the first time such intermediates have been seen in biology. Exo-glycal synthase TunA uses an elegantly subtle mechanism to control regioselectivity and with exo-glycal epimerase TunF sets a logical chemical stage for downstream radical C–C coupling.

    • Filip J. Wyszynski
    • , Seung Seo Lee
    •  & Benjamin G. Davis

  • Article |

    Macromolecules with antimicrobial properties are promising materials for combating multi-drug-resistant microbes. Now, it has been shown that amphiphilic cationic polycarbonates that are biodegradable can self-assemble into micellar nanoparticles that can kill gram-positive bacteria, MRSA and fungi efficiently, even at low concentrations. Moreover, no significant toxicity is observed during in vivo studies in mice.

    • Fredrik Nederberg
    • , Ying Zhang
    •  & Yi-Yan Yang

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