Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors

…, P O'Shea, C Lindholm, A Cockayne…

文献索引：Murray, Ewan J.; Crowley, Rebecca C.; Truman, Alex; Clarke, Simon R.; Cottam, James A.; Jadhav, Gopal P.; Steele, Victoria R.; O'Shea, Paul; Lindholm, Catharina; Cockayne, Alan; Chhabra, Siri Ram; Chan, Weng C.; Williams, Paul Journal of Medicinal Chemistry, 2014 , vol. 57, # 6 p. 2813 - 2819

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被引用次数: 30

摘要

A series of 3-oxo-C12-HSL, tetramic acid, and tetronic acid analogues were synthesized to gain insights into the structural requirements for quorum sensing inhibition in Staphylococcus aureus. Compounds active against agr were noncompetitive inhibitors of the autoinducing peptide (AIP) activated AgrC receptor, by altering the activation efficacy of the cognate AIP-1. They appeared to act as negative allosteric modulators and are ...