6-Polyaminosteroid Squalamine Analogues Display Antibacterial Activity against Resistant Pathogens.
Int J Mol Sci
; 24(10)2023 May 10.
Article
em En
| MEDLINE
| ID: mdl-37239913
ABSTRACT
A series of 6-polyaminosteroid analogues of squalamine were synthesized with moderate to good yields and evaluated for their in vitro antimicrobial properties against both susceptible and resistant Gram-positive (vancomycin-resistant Enterococcus faecium and methicillin-resistant Staphylococcus aureus) and Gram-negative (carbapenem-resistant Acinetobacter baumannii and Pseudomonas aeruginosa) bacterial strains. Minimum inhibitory concentrations against Gram-positive bacteria ranged from 4 to 16 µg/mL for the most effective compounds, 4k and 4n, and showed an additive or synergistic effect with vancomycin or oxacillin. On the other hand, the derivative 4f, which carries a spermine moiety like that of the natural trodusquemine molecule, was found to be the most active derivative against all the resistant Gram-negative bacteria tested, with an MIC value of 16 µg/mL. Our results suggest that 6-polyaminosteroid analogues of squalamine are interesting candidates for Gram-positive bacterial infection treatments, as well as potent adjuvants to fight Gram-negative bacterial resistance.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Staphylococcus aureus Resistente à Meticilina
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article