Evaluation of a focused library of N-aryl L-homoserine lactones reveals a new set of potent quorum sensing modulators

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:18

Article

Geske, Grant D.¹  Mattmann, Margrith E.¹  Blackwell, Helen E.¹ 

[1] Univ Wisconsin, Dept Chem, Madison, WI 53706 USA

关键词: AHL;    N-Acylated homoserine lactone;    Quorum sensing;   

DOI  :  10.1016/j.bmcl.2008.07.089

来源: Elsevier

【 摘 要 】

A focused library of N-aryl L-homoserine lactones was designed around known lactone leads and evaluated for antagonistic and agonistic activity against quorum-sensing receptors in Agrobacterium tumefaciens, Pseudomonas aeruginosa, and Vibrio fischeri. Several compounds were identified with significantly heightened activities relative to the lead compounds, and new structure-activity relationships (SARs) were delineated. Notably, 4-substituted N-phenoxyacetyl and 3-substituted N-phenylpropionyl L-homoserine lactones were identified as potent antagonists of TraR and LuxR, respectively. (C) 2008 Elsevier Ltd. All rights reserved.

【 授权许可】

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