Abstract
Novel pyrone-derived quorum sensing (QS) ligands to inhibit the binding of OdDHL to the LasR of Pseudomonas aeruginosa were designed, synthesized and evaluated. Among the analogs, the most potent compound 8 exhibited strong in vitro inhibitory activities against biofilm formation and down-regulated OdDHL/LasR-associated genes by 35-67%. The binding mode of 8 in silico was highly similar to that of the crystal ligand OdDHL in the active site of LasR.
| Original language | English |
|---|---|
| Pages (from-to) | 2913-2917 |
| Number of pages | 5 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 25 |
| Issue number | 15 |
| DOIs | |
| Publication status | Published - 2015 Mar 26 |
Keywords
- Biofilm inhibition
- Pseudomonas aeruginosa
- Pyrone
- Quorum sensing
ASJC Scopus subject areas
- Biochemistry
- Clinical Biochemistry
- Molecular Biology
- Molecular Medicine
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
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Park, S., Kim, H. S., Ok, K., Kim, Y., Park, H-D., & Byun, Y. (2015). Design, synthesis and biological evaluation of 4-(alkyloxy)-6-methyl-2H-pyran-2-one derivatives as quorum sensing inhibitors. Bioorganic and Medicinal Chemistry Letters, 25(15), 2913-2917. https://doi.org/10.1016/j.bmcl.2015.05.054