Peer-Reviewed Journal Details
Mandatory Fields
Moynihan, E;Mackey, K;Blaskovich, MAT;Reen, J;McGlacken, G
2022
August
Acs Medicinal Chemistry Letters
N-Alkyl-2-Quinolonopyrones Demonstrate Antimicrobial Activity against ESKAPE Pathogens Including Staphylococcus aureus
Validated
Scopus: 1 ()
Optional Fields
ANTIBIOTIC-RESISTANCE QUINOLONES ARYLATION VIRULENCE PALLADIUM PYRIDONES REVEALS SYSTEM
13
1358
1362
Antibiotic resistance has grown significantly in the last three decades, while research and development of new antibiotic classes has languished. Therefore, new chemical frameworks for the control of microbial behavior are urgently required. This study presents a novel suite of compounds, based on a tricyclic 4-hydroxy-2H-pyrano[3,2-c]quinoline-2,5(6H)-dione core, with significant antibiotic activity against the ESKAPE pathogens Staphylococcus aureus and Enterococcus faecalis and the "accidental pathogen" Staphylococcus epidermidis. A potent analogue with an N-heptyl-9-t-Bu substitution pattern emerged as a hit with MIC levels <= 2 mu g/mL across four strains of MRSA. In addition, the same compound proved highly potent against Enterococcus spp. (0.25 mu g/mL).
WASHINGTON
1948-5875
10.1021/acsmedchemlett.2c00185
Grant Details