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Assay Development for High-Throughput Drug Screening Against Mycobacteria
Published on: October 25, 2024
New bisanthraquinone antibiotics and semi-synthetic derivatives with potent activity against clinical Staphylococcus
Aaron M Socha1, Kerry L LaPlante, David C Rowley
1Department of Biomedical, University of Rhode Island, 53 Fogarty Hall Kingston, RI 02881, USA.
Abstract:
The escalation of antibiotic resistance among Gram-positive pathogens presents increasing treatment challenges and requires the development of innovative therapeutic agents. Here, we present the antimicrobial properties of structurally unusual bisanthraquinone metabolites produced by a marine streptomycete and four semi-synthetic derivatives. Biological activities were measured against clinically derived isolates of vancomycin-resistant Enterococcus faecium (VRE), and methicillin-susceptible, methicillin-resistant, and tetracycline-resistant Staphylococcus aureus (MSSA, MRSA, and TRSA, respectively). The most potent antibiotic displayed MIC(50) values of 0.11, 0.23, and 0.90microM against a panel (n=25 each) of clinical MSSA, MRSA, and VRE, respectively, and was determined to be bactericidal by time-kill analysis.
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