
pmid: 21782453
Thirty N,N'-disubstituted imidazolium salts have been synthesized and evaluated as LuxR antagonists. Substitution on one of the imidazolium nitrogen atoms includes benzhydryl, fluorenyl or cyclopentyl substituent, and alkyl chains of various lengths on the second one. Most of these compounds displayed antagonist activity, with IC(50) reaching the micromolar range for the most active ones. The disubstituted imidazolium scaffold is thus shown to be a new pertinent pharmacophore in the field of AHL dependent QS inhibition.
Models, Molecular, Nitrogen, Imidazoles, Quorum Sensing, Microbial Sensitivity Tests, [CHIM.ORGA] Chemical Sciences/Organic chemistry, Anti-Bacterial Agents, Repressor Proteins, Drug Design, Luminescent Measurements, Trans-Activators, Humans, Salts, Molecular Targeted Therapy, Protein Binding
Models, Molecular, Nitrogen, Imidazoles, Quorum Sensing, Microbial Sensitivity Tests, [CHIM.ORGA] Chemical Sciences/Organic chemistry, Anti-Bacterial Agents, Repressor Proteins, Drug Design, Luminescent Measurements, Trans-Activators, Humans, Salts, Molecular Targeted Therapy, Protein Binding
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