New bisanthraquinone antibiotics and semi-synthetic derivatives with potent activity against clinical Staphylococcus aureus and Enterococcus faecium isolates
Date of Original Version
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 MIC50 values of 0.11, 0.23, and 0.90 μM against a panel (n = 25 each) of clinical MSSA, MRSA, and VRE, respectively, and was determined to be bactericidal by time-kill analysis. © 2006 Elsevier Ltd. All rights reserved.
Bioorganic and Medicinal Chemistry
Socha, Aaron M., Kerry L. LaPlante, and David C. Rowley. "New bisanthraquinone antibiotics and semi-synthetic derivatives with potent activity against clinical Staphylococcus aureus and Enterococcus faecium isolates." Bioorganic and Medicinal Chemistry 14, 24 (2006): 8446-8454. doi:10.1016/j.bmc.2006.08.038.