Targeting Staphylococcus aureus Quorum Sensing with Nonpeptidic Small Molecule Inhibitors | Zendy

Ewan J. Murray | Zendy; Rebecca C. Crowley | Zendy; Alex Truman | Zendy; Simon R. Clarke | Zendy; James A. Cottam | Zendy; Gopal P. Jadhav | Zendy; Victoria R. Steele | Zendy; Paul O’Shea | Zendy; Catharina Lindholm | Zendy; Alan Cockayne | Zendy; Siri Ram Chhabra | Zendy; Weng C. Chan | Zendy; Paul Williams | Zendy

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Targeting Staphylococcus aureus Quorum Sensing with Nonpeptidic Small Molecule Inhibitors

Author(s) -

Ewan J. Murray,

Rebecca C. Crowley,

Alex Truman,

Simon R. Clarke,

James A. Cottam,

Gopal P. Jadhav,

Victoria R. Steele,

Paul O’Shea,

Catharina Lindholm,

Alan Cockayne,

Siri Ram Chhabra,

Weng C. Chan,

Paul Williams

Publication year - 2014

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm500215s

Subject(s) - quorum sensing , chemistry , allosteric regulation , staphylococcus aureus , small molecule , structure–activity relationship , stereochemistry , receptor , biochemistry , microbiology and biotechnology , combinatorial chemistry , bacteria , in vitro , virulence , biology , genetics , gene

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.

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