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Research output: Contribution to Journal/Magazine › Journal article › peer-review
Research output: Contribution to Journal/Magazine › Journal article › peer-review
}
TY - JOUR
T1 - Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors
AU - Murray, Ewan J.
AU - Crowley, Rebecca C.
AU - Truman, Alex
AU - Clarke, Simon R.
AU - Cottam, James A.
AU - Jadhav, Gopal P.
AU - Steele, Victoria R.
AU - O'Shea, Paul
AU - Lindholm, Catharina
AU - Cockayne, Alan
AU - Chhabra, Siri Ram
AU - Chan, Weng C.
AU - Williams, Paul
PY - 2014/3/27
Y1 - 2014/3/27
N2 - 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 exemplified by 3-tetradecanoyltetronic acid 17, which reduced nasal cell colonization and arthritis in a murine infection model.
AB - 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 exemplified by 3-tetradecanoyltetronic acid 17, which reduced nasal cell colonization and arthritis in a murine infection model.
U2 - 10.1021/jm500215s
DO - 10.1021/jm500215s
M3 - Journal article
C2 - 24592914
VL - 57
SP - 2813
EP - 2819
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 3
ER -