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Re-evolution of the 2-phenylquinolines: Ligand-based design, synthesis, and biological evaluation of a potent new class of staphylococcus aureus NorA efflux pump inhibitors to combat antimicrobial resistance
Overexpression of efflux pumps is an important mechanism by which bacteria evade the effects of antimicrobial agents that are substrates. NorA is a Staphylococcus aureus efflux pump that confers reduced susceptibility to many structurally unrelated agents, including fluoroquinolones, biocides, and dyes, resulting in a multidrug resistant (MDR) phenotype. In this work, a series of 2-phenylquinoline derivatives was designed by means of ligand-based pharmacophore modeling in an attempt to identify improved S. aureus NorA efflux pump inhibitors (EPIs). Most of the 2-phenylquinoline derivatives displayed potent EPI activity against the norA overexpressing strain SA-1199B. The antibacterial activity of ciprofloxacin, when used in combination with some of the synthesized compounds, was completely restored in SA-1199B and SA-K2378, a strain overexpressing norA from a multicopy plasmid. Compounds 3m and 3q also showed potent synergistic activity with the ethidium bromide dye in a strain overexpressing the MepA MDR efflux pump.
Because enzymes can increase reaction rates by enormous factors and tend to be very specific, SDS of cas: 177-11-7, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 177-11-7
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Piperidine – Wikipedia,
Piperidine | C5H7517N – PubChem