Synthesis and biological activity of N-Acylated ornithine analogues of daptomycin.
N-Acylated ornithine analogues of daptomycin were synthesized and tested for their antibacterial efficacy.
Animals↗
Biomedical subjects
Valerie Laganas
Publications and source records attributed to Valerie Laganas.
Array synthesis of novel lipodepsipeptide.
Synthetic array technology was utilized to rapidly synthesize and analyze a diverse set of reductive alkylation analogues of daptomycin. Analysis of the array suggested the use of polar functionality such as sulfonamides or amide or polar spaces such as piperazine would beneficially affect activity.
Alkylation↗
In vitro bactericidal activities of daptomycin against Staphylococcus aureus and Enterococcus faecalis are not mediated by inhibition of lipoteichoic acid biosynthesis.
Previous studies have suggested that lipoteichoic acid biosynthesis inhibition is the mechanism of action of daptomycin. In this investigation, daptomycin inhibited all macromolecular synthesis in Staphylococcus aureus, Enterococcus faecalis, and Enterococcus hirae without kinetic or dose specificity for lipoteichoic acid. Daptomycin remained bactericidal in the absence of ongoing lipoteichoic acid synthesis. Inhibition of lipoteichoic acid synthesis is apparently not the mechanism of action of daptomycin in these pathogens.
Anti-Bacterial Agents↗