Abstract
A series of lipophilic teicoplanin pseudoaglycon derivatives, including alkyl-, aryl-, calixarene- and protected sugar-containing conjugates, were prepared using azide–alkyne click chemistry. Out of the conditions applied, the CuSO4–ascorbate reagent system proved to be more efficient than the Cu(I)I–Et3N-mediated reaction. Some of the new compounds have high in vitro activity against glycopeptide-resistant Gram-positive bacteria, including vanA-positive Enterococcus faecalis. A few of them also display promising in vitro anti-influenza activity.
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Acknowledgements
We thank the financial support from the Hungarian Research Fund (OTKA K 109208). This research was also supported by the European Union and the State of Hungary, co-financed by the European Social Fund in the framework of TÁMOP-4.2.2B-15/1/KONV-2015-0001.
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Szűcs, Z., Csávás, M., Rőth, E. et al. Synthesis and biological evaluation of lipophilic teicoplanin pseudoaglycon derivatives containing a substituted triazole function. J Antibiot 70, 152–157 (2017). https://doi.org/10.1038/ja.2016.80
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DOI: https://doi.org/10.1038/ja.2016.80
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