Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors

Bioorganic & Medicinal Chemistry
2008.0

Abstract

Based on our recent findings that piperine is a potent Staphylococcus aureus NorA efflux pump inhibitor (EPI), 38 piperine analogs were synthesized and bioevaluated for their EPI activity. Twenty-five of them were found active with potentiating activity equivalent or more than known EPIs like reserpine, carsonic acid and verapamil. The inhibitory mechanism of the compounds was confirmed by efflux inhibition assay using ethidium bromide as NorA substrate. The present communication describes the synthesis, bioevaluation and structure related activity of these efflux pump inhibitors.

Knowledge Graph

Similar Paper

Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors
Bioorganic & Medicinal Chemistry 2008.0
Amino acid amides of piperic acid (PA) and 4-ethylpiperic acid (EPA) as NorA efflux pump inhibitors of Staphylococcus aureus
Bioorganic & Medicinal Chemistry Letters 2016.0
Synthesis of amides from (E)-3-(1-chloro-3,4-dihydronaphthalen-2-yl)acrylic acid and substituted amino acid esters as NorA efflux pump inhibitors of Staphylococcus aureus
Bioorganic & Medicinal Chemistry 2019.0
Citral derived amides as potent bacterial NorA efflux pump inhibitors
Bioorganic & Medicinal Chemistry 2008.0
Chalcone inhibitors of the NorA efflux pump in Staphylococcus aureus whole cells and enriched everted membrane vesicles
Bioorganic & Medicinal Chemistry 2012.0
N-Caffeoylphenalkylamide derivatives as bacterial efflux pump inhibitors
Bioorganic & Medicinal Chemistry Letters 2007.0
Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus
European Journal of Medicinal Chemistry 2010.0
From Phenothiazine to 3-Phenyl-1,4-benzothiazine Derivatives as Inhibitors of theStaphylococcus aureusNorA Multidrug Efflux Pump
Journal of Medicinal Chemistry 2008.0
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
Journal of Medicinal Chemistry 2013.0
Synthesis of Omeprazole Analogues and Evaluation of These as Potential Inhibitors of the Multidrug Efflux Pump NorA ofStaphylococcus aureus
Antimicrobial Agents and Chemotherapy 2007.0