N-Terminal guanidine derivatives of teicoplanin antibiotics strongly active against glycopeptide resistant Enterococcus faecium.
Anti-Bacterial Agents
/ pharmacology
Drug Resistance, Microbial
/ drug effects
Enterococcus faecium
/ drug effects
Glycopeptides
/ pharmacology
Gram-Positive Bacteria
/ drug effects
Gram-Positive Bacterial Infections
/ drug therapy
Guanidines
/ pharmacology
Humans
Microbial Sensitivity Tests
/ methods
Teicoplanin
/ pharmacology
Journal
The Journal of antibiotics
ISSN: 1881-1469
Titre abrégé: J Antibiot (Tokyo)
Pays: England
ID NLM: 0151115
Informations de publication
Date de publication:
09 2020
09 2020
Historique:
received:
24
02
2020
accepted:
15
04
2020
revised:
26
03
2020
pubmed:
16
5
2020
medline:
29
12
2020
entrez:
16
5
2020
Statut:
ppublish
Résumé
Antibiotic resistance is one of the major challenges in healthcare of our time. To meet this challenge, we designed and prepared guanidine and lipophilic guanidine derivatives of the glycopeptide antibiotic teicoplanin to armed them with activity against the most threatening nosocomial bacteria, multiresistant enterococci. From teicoplanin and its pseudoaglycone, a series of N-terminal guanidine derivatives have been prepared with free and amide C-terminal parts. Six aliphatic and aromatic lipophilic carbodiimides were prepared and used for the synthesis of lipophilic guanidine teicoplanin conjugates. All new N-terminal guanidine antibiotics showed high activity against a standard panel of Gram-positive bacteria. Four selected derivatives displayed excellent antibacterial activity against a series of nosocomial VanA Enterococcus faecium strains.
Identifiants
pubmed: 32409678
doi: 10.1038/s41429-020-0313-6
pii: 10.1038/s41429-020-0313-6
doi:
Substances chimiques
Anti-Bacterial Agents
0
Glycopeptides
0
Guanidines
0
Teicoplanin
61036-62-2
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
603-614Références
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