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 |
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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
Cite this
Design, synthesis and biological evaluation of 4-(alkyloxy)-6-methyl-2H-pyran-2-one derivatives as quorum sensing inhibitors. / Park, Suzie; Kim, Han Shin; Ok, Kiwon; Kim, Yunhye; Park, Hee-Deung; Byun, Youngjoo.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 25, No. 15, 26.03.2015, p. 2913-2917.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Design, synthesis and biological evaluation of 4-(alkyloxy)-6-methyl-2H-pyran-2-one derivatives as quorum sensing inhibitors
AU - Park, Suzie
AU - Kim, Han Shin
AU - Ok, Kiwon
AU - Kim, Yunhye
AU - Park, Hee-Deung
AU - Byun, Youngjoo
PY - 2015/3/26
Y1 - 2015/3/26
N2 - 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.
AB - 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.
KW - Biofilm inhibition
KW - Pseudomonas aeruginosa
KW - Pyrone
KW - Quorum sensing
UR - http://www.scopus.com/inward/record.url?scp=84930924160&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84930924160&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2015.05.054
DO - 10.1016/j.bmcl.2015.05.054
M3 - Article
VL - 25
SP - 2913
EP - 2917
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 15
ER -