期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 15, 页码 4321-4324出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.06.090
关键词
quorum sensing; AHLs; LuxR; antagonist; V. fischeri; molecular modelling; docking
New N-acyl homoserine lactone analogues, N-acyl-3-amino-5H-furanone derivatives and some 4-halogeno counterparts, were synthesised and tested for their ability to modulate LuxR-dependent bacterial quorum sensing. Both types of analogues proved to be inhibitors, the halogenated compounds being significantly more active. Molecular modelling suggested that the conjugated enamide group induces two preferential conformations leading to specific binding modes. In addition, the presence of the halogen atom could enhance the fitting of the lactone ring through specific interactions with strictly conserved or conservatively replaceable residues in the LuxR protein family, namely Asp79, Trp94 and Ile81. (c) 2008 Elsevier Ltd. All rights reserved.
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