Design of membrane targeting tobramycin-based cationic amphiphiles with reduced hemolytic activity

Tobramycin-based cationic amphiphiles differing in the chemical bond linking their hydrophobic and hydrophilic parts were synthesized and biologically evaluated. Several compounds demonstrated potent antimicrobial activities compared to the parent drug. One analogue exhibited a significant reduction...

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Veröffentlicht in:MedChemComm 2013, Vol.4 (1), p.120-124
Hauptverfasser: Herzog, Ido M., Feldman, Mark, Eldar-Boock, Anat, Satchi-Fainaro, Ronit, Fridman, Micha
Format: Artikel
Sprache:eng
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Zusammenfassung:Tobramycin-based cationic amphiphiles differing in the chemical bond linking their hydrophobic and hydrophilic parts were synthesized and biologically evaluated. Several compounds demonstrated potent antimicrobial activities compared to the parent drug. One analogue exhibited a significant reduction in red blood cells hemolysis, demonstrating that it is possible to maintain the antimicrobial potency of these molecules while reducing their undesired hemolytic effect through chemical modifications.
ISSN:2040-2503
2040-2511
DOI:10.1039/C2MD20162C