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.
ASJC Scopus subject areas
- Drug Discovery