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.
MeSH terms
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Alkaloids / chemical synthesis
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Alkaloids / chemistry*
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Alkaloids / pharmacology*
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Anti-Bacterial Agents / chemistry*
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Anti-Bacterial Agents / pharmacology*
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Bacterial Proteins / antagonists & inhibitors*
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Bacterial Proteins / metabolism
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Benzodioxoles / chemical synthesis
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Benzodioxoles / chemistry*
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Benzodioxoles / pharmacology*
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Ciprofloxacin / chemistry
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Ciprofloxacin / pharmacology
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Enzyme Inhibitors / pharmacology
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Ethidium / metabolism
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Microbial Sensitivity Tests
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Multidrug Resistance-Associated Proteins / antagonists & inhibitors*
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Multidrug Resistance-Associated Proteins / metabolism
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Nucleic Acid Synthesis Inhibitors / chemistry
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Nucleic Acid Synthesis Inhibitors / pharmacology
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Piperidines / chemical synthesis
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Piperidines / chemistry*
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Piperidines / pharmacology*
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Polyunsaturated Alkamides / chemical synthesis
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Polyunsaturated Alkamides / chemistry*
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Polyunsaturated Alkamides / pharmacology*
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Staphylococcus aureus / drug effects*
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Staphylococcus aureus / metabolism
Substances
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Alkaloids
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Anti-Bacterial Agents
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Bacterial Proteins
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Benzodioxoles
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Enzyme Inhibitors
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Multidrug Resistance-Associated Proteins
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Nucleic Acid Synthesis Inhibitors
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Piperidines
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Polyunsaturated Alkamides
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NorA protein, Staphylococcus
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Ciprofloxacin
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Ethidium
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piperine