title: Synthesis and biological evaluation of lipophilic teicoplanin pseudoaglycon derivatives containing a substituted triazole function.
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.
authors.affiliation: Department of Pharmaceutical Chemistry, University of Debrecen, Debrecen, Hungary.
authors.forename: Zsolt
authors.initials: Z
authors.lastname: Szűcs
authors.affiliation: Department of Pharmaceutical Chemistry, University of Debrecen, Debrecen, Hungary.
authors.forename: Magdolna
authors.initials: M
authors.lastname: Csávás
authors.affiliation: Department of Pharmaceutical Chemistry, University of Debrecen, Debrecen, Hungary.
authors.forename: Erzsébet
authors.initials: E
authors.lastname: Rőth
authors.affiliation: Department of Pharmaceutical Chemistry, University of Debrecen, Debrecen, Hungary.
authors.forename: Anikó
authors.initials: A
authors.lastname: Borbás
authors.affiliation: Department of Organic Chemistry, University of Debrecen, Debrecen, Hungary.
authors.forename: Gyula
authors.initials: G
authors.lastname: Batta
authors.affiliation: ICBMS-Equipe CSAp, Université Lyon 1, Villeurbanne, France.
authors.forename: Florent
authors.initials: F
authors.lastname: Perret
authors.affiliation: Department of Medical Microbiology, Semmelweis University, Budapest, Hungary.
authors.forename: Eszter
authors.initials: E
authors.lastname: Ostorházi
authors.affiliation: Department of Medical Microbiology, Semmelweis University, Budapest, Hungary.
authors.forename: Réka
authors.initials: R
authors.lastname: Szatmári
authors.affiliation: Rega Institute for Medical Research, KU Leuven, Leuven, Belgium.
authors.forename: Evelien
authors.initials: E
authors.lastname: Vanderlinden
authors.affiliation: Rega Institute for Medical Research, KU Leuven, Leuven, Belgium.
authors.forename: Lieve
authors.initials: L
authors.lastname: Naesens
authors.affiliation: Department of Pharmaceutical Chemistry, University of Debrecen, Debrecen, Hungary.
authors.forename: Pál
authors.initials: P
authors.lastname: Herczegh
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D024881:Drug Resistance, Bacterial; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D017334:Teicoplanin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D014230:Triazoles; D017334:Teicoplanin