Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors
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 Agr...
| Main Authors: | , , , , , , , , , , , , |
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| Format: | Article |
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American Chemical Society
2014
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| Online Access: | https://eprints.nottingham.ac.uk/37554/ |
| _version_ | 1848795483077607424 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Murray, Ewan J. |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | 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. |
| first_indexed | 2025-11-14T19:32:48Z |
| format | Article |
| id | nottingham-37554 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T19:32:48Z |
| publishDate | 2014 |
| publisher | American Chemical Society |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-375542020-05-04T16:44:14Z https://eprints.nottingham.ac.uk/37554/ Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors 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 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. American Chemical Society 2014-03-27 Article PeerReviewed 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. and Williams, Paul (2014) Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors. Journal of Medicinal Chemistry, 57 (6). pp. 2813-2819. ISSN 1520-4804 http://pubs.acs.org/doi/abs/10.1021/jm500215s doi:10.1021/jm500215s doi:10.1021/jm500215s |
| spellingShingle | 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 Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors |
| title | Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors |
| title_full | Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors |
| title_fullStr | Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors |
| title_full_unstemmed | Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors |
| title_short | Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors |
| title_sort | targeting staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors |
| url | https://eprints.nottingham.ac.uk/37554/ https://eprints.nottingham.ac.uk/37554/ https://eprints.nottingham.ac.uk/37554/ |