Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591758 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
Abstract
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.
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Authors
Adam R. Benoit, Charles Schiaffo, Christine E. Salomon, John R. Goodell, Hiroshi Hiasa, David M. Ferguson,