Synthesis and evaluation of N-alkyl-9-aminoacridines with antibacterial activity

AR Benoit, C Schiaffo, CE Salomon, JR Goodell…

Index: Benoit, Adam R.; Schiaffo, Charles; Salomon, Christine E.; Goodell, John R.; Hiasa, Hiroshi; Ferguson, David M. Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 14 p. 3014 - 3017

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Citation Number: 9

Abstract

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 MIC 99 values of 2–3 μM for alkyl chains ranging from 10 to 14 carbons in length. Although prior ...