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Synthesis and biological evaluation of zinc chelating compounds as metallo-β-lactamase inhibitorsElectronic supplementary information (ESI) available: Synthetic details, NMR spectra and intrinsic bacterial activity of chelators. See DOI: 10.1039/c8md00578h

Kildahl-Andersen, Geir et al.

MedChemComm: rapid communication of research in medicinal chemistry. Volume 10:Issue 4 (2019); pp 528-537 -- Royal Society of Chemistry

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  • Title:
    Synthesis and biological evaluation of zinc chelating compounds as metallo-β-lactamase inhibitorsElectronic supplementary information (ESI) available: Synthetic details, NMR spectra and intrinsic bacterial activity of chelators. See DOI: 10.1039/c8md00578h
  • Author: Kildahl-Andersen, Geir;
    Schnaars, Christian;
    Prandina, Anthony;
    Radix, Sylvie;
    Le Borgne, Marc;
    Jordheim, Lars Petter;
    Gjøen, Tor;
    Andresen, Adriana Magalhães Santos;
    Lauksund, Silje;
    Fröhlich, Christopher;
    Samuelsen, Ørjan;
    Rongved, Pål;
    Åstrand, Ove Alexander Høgmoen
  • Found In: MedChemComm: rapid communication of research in medicinal chemistry. Volume 10:Issue 4 (2019); pp 528-537
  • Journal Title: MedChemComm: rapid communication of research in medicinal chemistry
  • Subjects: Pharmaceutical chemistry--Periodicals; Dewey: 615.19
  • Rights: Licensed
  • Publication Details: Royal Society of Chemistry
  • Abstract:

    The syntheses of metallo-β-lactamase inhibitors comprising chelating moieties, with varying zinc affinities, and peptides partly inspired from bacterial peptide sequences, have been undertaken. The zinc chelator strength was varied using the following chelators, arranged in order of ascending binding affinity: dipicolylamine (DPA, tridentate), dipicolyl-1, 2, 3-triazolylmethylamine (DPTA, tetradentate) dipicolyl ethylenediamine (DPED, tetradentate) and trispicolyl ethylenediamine (TPED, pentadentate). The chosen peptides were mainly based on the known sequence of the C-terminus of the bacterial peptidoglycan precursors. Biological evaluation on clinical bacterial isolates, harbouring either the NDM-1 or VIM-2 metallo-β-lactamase, showed a clear relationship between the zinc chelator strength and restoration of meropenem activity. However, evaluation of toxicity on different cancer cell lines demonstrated a similar trend, and thus inclusion of the bacterial peptides did possess rather high toxicity towards eukaryotic cells.


  • Identifier: System Number: ETOCvdc_100080328452.0x000001; Journal ISSN: 2040-2503; 10.1039/c8md00578h
  • Publication Date: 2019
  • Physical Description: Electronic
  • Shelfmark(s): 5424.685000
  • UIN: ETOCvdc_100080328452.0x000001

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