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2 results on '"Benzyloxy-2-phenylquinoline derivatives"'

1. Studies on 2-phenylquinoline Staphylococcus aureus NorA efflux pump inhibitors: New insights on the C-6 position.

Author

Felicetti, Tommaso, Cannalire, Rolando, Nizi, Maria Giulia, Tabarrini, Oriana, Massari, Serena, Barreca, Maria Letizia, Manfroni, Giuseppe, Schindler, Bryan D., Cecchetti, Violetta, Kaatz, Glenn W., and Sabatini, Stefano

Subjects
*STAPHYLOCOCCUS aureus, *ANTI-infective agents, *DRUG resistance in bacteria, *DRUG resistance, *DOSAGE forms of drugs, *METHICILLIN-resistant staphylococcus aureus
Abstract

The alarming and rapid spread of antimicrobial resistance among bacteria represents a high risk for global health. Targeting factors involved in resistance to restore the activity of failing antibiotics is a promising strategy to overcome this urgent medical need. Efflux pump inhibitors are able to increase antibiotic concentrations in bacteria, thus they can be considered true antimicrobial resistance breakers. In this work, continuing our studies on inhibitors of the Staphylococcus aureus NorA pump, we designed, synthesized and biologically evaluated novel 2-phenylquinoline derivatives starting from our hits 1 and 2 . Two of the synthesized compounds ( 6 and 7 ) bearing a C-6 benzyloxy group showed the best NorA inhibition activity, thereby providing an excellent starting point to direct future chemical optimizations. [ABSTRACT FROM AUTHOR]

Published
2018
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2. Studies on 2-phenylquinoline Staphylococcus aureus NorA efflux pump inhibitors: New insights on the C-6 position

Author

Stefano Sabatini, Oriana Tabarrini, Maria Letizia Barreca, Bryan D. Schindler, Giuseppe Manfroni, Violetta Cecchetti, Tommaso Felicetti, Rolando Cannalire, Maria Giulia Nizi, Serena Massari, Glenn W. Kaatz, Felicetti, T., Cannalire, R., Nizi, M. G., Tabarrini, O., Massari, S., Barreca, M. L., Manfroni, G., Schindler, B. D., Cecchetti, V., Kaatz, G. W., and Sabatini, S.

Subjects
0301 basic medicine, Staphylococcus aureus, Cell Survival, medicine.drug_class, 030106 microbiology, Antibiotics, Benzyloxy-2-phenylquinoline derivatives, NorA efflux pump, Microbial Sensitivity Tests, Pharmacology, medicine.disease_cause, Antimicrobial resistance, 01 natural sciences, Structure-Activity Relationship, 03 medical and health sciences, Antibiotic resistance, Bacterial Proteins, Drug Discovery, medicine, Humans, Efflux pump inhibitors, NorA efflux pump, Staphylococcus aureus, Benzyloxy-2-phenylquinoline derivatives, Antimicrobial resistance, Antibiotic resistance breakers, Efflux pump inhibitors, Dose-Response Relationship, Drug, Molecular Structure, 2-phenylquinoline, biology, Chemistry, Organic Chemistry, Antibiotic resistance breakers, Hep G2 Cells, General Medicine, biology.organism_classification, Benzyloxy-2-phenylquinoline derivative, Anti-Bacterial Agents, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Quinolines, Staphylococcus aureu, Efflux, Multidrug Resistance-Associated Proteins, Bacteria, Efflux pump inhibitor
Abstract

The alarming and rapid spread of antimicrobial resistance among bacteria represents a high risk for global health. Targeting factors involved in resistance to restore the activity of failing antibiotics is a promising strategy to overcome this urgent medical need. Efflux pump inhibitors are able to increase antibiotic concentrations in bacteria, thus they can be considered true antimicrobial resistance breakers. In this work, continuing our studies on inhibitors of the Staphylococcus aureus NorA pump, we designed, synthesized and biologically evaluated novel 2-phenylquinoline derivatives starting from our hits 1 and 2. Two of the synthesized compounds (6 and 7) bearing a C-6 benzyloxy group showed the best NorA inhibition activity, thereby providing an excellent starting point to direct future chemical optimizations.

Published
2018

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