Conjugates of Ciprofloxacin and Amphiphilic Block Copoly(2-alkyl-2-oxazolines)s Overcome Efflux Pumps and Are Active against CIP-Resistant Bacteria.
Anti-Bacterial Agents
/ chemistry
Cells, Cultured
Ciprofloxacin
/ chemistry
Drug Compounding
/ methods
Drug Resistance, Bacterial
Escherichia coli
/ drug effects
Excipients
/ chemistry
Humans
Mesenchymal Stem Cells
Microbial Sensitivity Tests
Oxazoles
/ chemistry
Staphylococcus aureus
/ drug effects
amphiphilic polymers
bacterial resistances
ciprofloxacin
efflux pumps
hydrophobic/hydrophilic balance (HHB)
poly(2-oxazolines)
polymer−antibiotic conjugate
Journal
Molecular pharmaceutics
ISSN: 1543-8392
Titre abrégé: Mol Pharm
Pays: United States
ID NLM: 101197791
Informations de publication
Date de publication:
06 09 2021
06 09 2021
Historique:
pubmed:
30
7
2021
medline:
28
1
2022
entrez:
29
7
2021
Statut:
ppublish
Résumé
Conjugation of antibiotics with polymers is an emerging strategy to improve the performance of these important drugs. Here, the antibiotic ciprofloxacin (CIP) was conjugated with amphiphilic poly(2-oxazoline) (POx) block copolymers to investigate whether the activity of the antibiotic was enhanced due to additionally induced membrane activity. The resulting polymer-antibiotic conjugates (PACs) are an order of magnitude more active against the bacterial strain
Identifiants
pubmed: 34323492
doi: 10.1021/acs.molpharmaceut.1c00430
doi:
Substances chimiques
Anti-Bacterial Agents
0
Excipients
0
Oxazoles
0
poly(2-oxazoline)
0
Ciprofloxacin
5E8K9I0O4U
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM