Synthesis and biological evaluation of lipophilic teicoplanin pseudoaglycon derivatives containing a substituted triazole function

Zsolt Szucs, Magdolna Csávás, Erzsébet Roth, Anikó Borbás, G. Batta, Florent Perret, Eszter Ostorházi, Réka Szatmári, Evelien Vanderlinden, Lieve Naesens, Pál Herczegh

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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 CuSO 4-ascorbate reagent system proved to be more efficient than the Cu(I)I-Et 3 N-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.

Original languageEnglish
Pages (from-to)152-157
Number of pages6
JournalJournal of Antibiotics
Volume70
Issue number2
DOIs
Publication statusPublished - Feb 1 2017

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ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

Cite this

Szucs, Z., Csávás, M., Roth, E., Borbás, A., Batta, G., Perret, F., Ostorházi, E., Szatmári, R., Vanderlinden, E., Naesens, L., & Herczegh, P. (2017). Synthesis and biological evaluation of lipophilic teicoplanin pseudoaglycon derivatives containing a substituted triazole function. Journal of Antibiotics, 70(2), 152-157. https://doi.org/10.1038/ja.2016.80