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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Benoit AR,Schiaffo C,Salomon CE,Goodell JR,Hiasa H,Ferguson DM

doi

10.1016/j.bmcl.2014.05.037

subject

Has Abstract

pub_date

2014-07-15 00:00:00

pages

3014-7

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00537-X

journal_volume

24

pub_type

杂志文章

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