Abstract
A focused library of N-aryl l-homoserine lactones was designed around known lactone leads and evaluated for antagonistic and agonistic activity against quorum-sensing receptors in Agrobacterium tumefaciens, Pseudomonas aeruginosa, and Vibrio fischeri. Several compounds were identified with significantly heightened activities relative to the lead compounds, and new structure-activity relationships (SARs) were delineated. Notably, 4-substituted N-phenoxyacetyl and 3-substituted N-phenylpropionyl l-homoserine lactones were identified as potent antagonists of TraR and LuxR, respectively.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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4-Butyrolactone / analogs & derivatives*
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4-Butyrolactone / chemical synthesis
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4-Butyrolactone / chemistry
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4-Butyrolactone / pharmacology
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Agrobacterium tumefaciens / metabolism
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Aliivibrio fischeri / metabolism
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Bacterial Proteins / antagonists & inhibitors
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Combinatorial Chemistry Techniques
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Dose-Response Relationship, Drug
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Molecular Structure
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Pseudomonas aeruginosa / metabolism
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Quorum Sensing / drug effects*
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Repressor Proteins / antagonists & inhibitors
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Structure-Activity Relationship
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Trans-Activators / antagonists & inhibitors
Substances
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Bacterial Proteins
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Repressor Proteins
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TraR protein, Agrobacterium tumefaciens
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Trans-Activators
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LuxR autoinducer binding proteins
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homoserine lactone
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4-Butyrolactone