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N-Acyl-3-amino-5H-furanone derivatives as new inhibitors of LuxR-dependent quorum sensing: Synthesis, biological evaluation and binding mode study

J Estephane, J Dauvergne, L Soulère…

文献索引:Estephane, Jane; Dauvergne, Julien; Soulere, Laurent; Reverchon, Sylvie; Queneau, Yves; Doutheau, Alain Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 15 p. 4321 - 4324

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被引用次数: 34

摘要

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 ...