Journal
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Volume 24, Issue 10, Pages -Publisher
MDPI
DOI: 10.3390/ijms24108568
Keywords
aminosteroid derivatives; polyamine; antimicrobial activities; Acinetobacter baumannii; Pseudomonas aeruginosa; Staphylococcus aureus; Enterococcus faecium
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A series of 6-polyaminosteroid analogues of squalamine were synthesized and evaluated for their antimicrobial properties against susceptible and resistant bacteria strains. The compounds showed promising activity against Gram-positive bacteria and strong activity against resistant Gram-negative bacteria. These analogues have the potential to be used as treatments for Gram-positive bacterial infections and as adjuvants to combat Gram-negative bacterial resistance.
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 mu g/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 mu g/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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