학술논문
6-Polyaminosteroid Squalamine Analogues Display Antibacterial Activity against Resistant Pathogens.
Document Type
Article
Author
Source
Subject
*CARBAPENEM-resistant bacteria
*ENTEROCOCCUS faecium
*ACINETOBACTER baumannii
*ANTIBACTERIAL agents
*ENTEROCOCCUS
*METHICILLIN-resistant staphylococcus aureus
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Language
ISSN
1661-6596
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. [ABSTRACT FROM AUTHOR]