Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors

…, P O'Shea, C Lindholm, A Cockayne…

Index: 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

Full Text: HTML

Citation Number: 30

Abstract

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 ...

Related Articles:

Regio-and stereoselective ring opening of. OMEGA.-alkenyllactones using organocopper reagents.

[Kawashima, Masatoshi; Sato, Toshio; Fujisawa, Tamotsu Bulletin of the Chemical Society of Japan, 1988 , vol. 61, p. 3255 - 3264]

Simple methods for the syntheses of (E)-4-and (E)-5-alkenoic acids by the SN2′ type reactions of γ-vinyl-γ-butyrolactone and δ-vinyl-δ-valerolactone with …

[Fujisawa, Tamotsu; Sato, Toshio; Kawashima, Masatoshi; Naruse, Kouichi; Tamai, Kouichi Tetrahedron Letters, 1982 , vol. 23, # 35 p. 3583 - 3586]

Stereochemically controlled synthesis of unsaturated acids via diphenylphosphinoyl (Ph 2 PO)-ketoacids

[Levin, Daniel; Warren, Stuart Tetrahedron Letters, 1985 , vol. 26, # 4 p. 505 - 508]

Simple methods for the syntheses of (E)-4-and (E)-5-alkenoic acids by the SN2′ type reactions of γ-vinyl-γ-butyrolactone and δ-vinyl-δ-valerolactone with …

[Fujisawa, Tamotsu; Sato, Toshio; Kawashima, Masatoshi; Naruse, Kouichi; Tamai, Kouichi Tetrahedron Letters, 1982 , vol. 23, # 35 p. 3583 - 3586]

A simple, general distereoselective synthesis of 5-hydroxyalkylbutan-4-olides

[Jefford, Charles W.; Wang, Ying Journal of the Chemical Society, Chemical Communications, 1987 , # 20 p. 1513 - 1514]

More Articles...