A series of 9-alkylaminoacridines were synthesized and evaluated for activity against two strains of methicillin-resistant and one strain of methicillin-sensitive Staphylococcus aureus. Results are presented that show a clear structure activity relationship between the N-alkyl chain length and antibacterial activity with peak MIC99 values of 2-3 μM for alkyl chains ranging from 10 to 14 carbons in length. Although prior work has linked the function of acridine-based compounds to intercalation and topoisomerase inhibition, the present results show that 9-alkylaminoacridines likely function as amphiphilic membrane-active disruptors potentially in a similar manner as quaternary ammonium antimicrobials. © 2014 Elsevier Ltd. All rights reserved.
CITATION STYLE
Benoit, A. R., Schiaffo, C., Salomon, C. E., Goodell, J. R., Hiasa, H., & Ferguson, D. M. (2014). Synthesis and evaluation of N-alkyl-9-aminoacridines with antibacterial activity. Bioorganic and Medicinal Chemistry Letters, 24(14), 3014–3017. https://doi.org/10.1016/j.bmcl.2014.05.037
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