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Full-Text Articles in Physical Sciences and Mathematics
Berberine-Inf55 (5-Nitro-2-Phenylindole) Hybrid Antimicrobials: Effects Of Varying The Relative Orientation Of The Berberine And Inf55 Components, Danuta Tomkiewicz, Gabriele Casadei, Jonah Larkins-Ford, Terence I. Moy, James A. Garner, John B. Bremner, Frederik M. Ausubel, Kim Lewis, Michael J. Kelso
Berberine-Inf55 (5-Nitro-2-Phenylindole) Hybrid Antimicrobials: Effects Of Varying The Relative Orientation Of The Berberine And Inf55 Components, Danuta Tomkiewicz, Gabriele Casadei, Jonah Larkins-Ford, Terence I. Moy, James A. Garner, John B. Bremner, Frederik M. Ausubel, Kim Lewis, Michael J. Kelso
Kim Lewis
Hybrid antimicrobials containing an antibacterial linked to a multidrug resistance (MDR) pump inhibitor make up a promising new class of agents for countering efflux-mediated bacterial drug resistance. This study explores the effects of varying the relative orientation of the antibacterial and efflux pump inhibitor components in three isomeric hybrids (SS14, SS14-M, and SS14-P) which link the antibacterial alkaloid and known substrate for the NorA MDR pump berberine to different positions on INF55 (5-nitro-2-phenylindole), an inhibitor of NorA. The MICs for all three hybrids against wild-type, NorA-knockout, and NorA-overexpressing Staphylococcus aureus cells were found to be similar (9.4 to 40.2 mu …