| Autor: |
Meschwitz SM; Department of Chemistry, Salve Regina University, Newport, RI 02840, USA. susan.meschwitz@salve.edu., Teasdale ME; Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI 02881, USA., Mozzer A; Department of Chemistry, Salve Regina University, Newport, RI 02840, USA., Martin N; Department of Chemistry, Salve Regina University, Newport, RI 02840, USA., Liu J; Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI 02881, USA., Forschner-Dancause S; Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI 02881, USA., Rowley DC; Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI 02881, USA. drowley@uri.edu. |
| Abstrakt: |
Quorum sensing (QS) antagonists have been proposed as novel therapeutic agents to combat bacterial infections. We previously reported that the secondary metabolite 3-methyl- N -(2'-phenylethyl)-butyramide, produced by a marine bacterium identified as Halobacillus salinus , inhibits QS controlled phenotypes in multiple Gram-negative reporter strains. Here we report that N -phenethyl hexanamide, a structurally-related compound produced by the marine bacterium Vibrio neptunius , similarly demonstrates QS inhibitory properties. To more fully explore structure-activity relationships within this new class of QS inhibitors, a panel of twenty analogs was synthesized and biologically evaluated. Several compounds were identified with increased attenuation of QS-regulated phenotypes, most notably N -(4-fluorophenyl)-3-phenylpropanamide against the marine pathogen Vibrio harveyi (IC 50 = 1.1 µM). These findings support the opportunity to further develop substituted phenethylamides as QS inhibitors. |
