Targeting Staphylococcus aureus quorum sensing with nonpeptidic small molecule inhibitors.
J Med Chem
; 57(6): 2813-9, 2014 Mar 27.
Article
em En
| MEDLINE
| ID: mdl-24592914
ABSTRACT
A series of 3-oxo-C12-HSL, tetramic acid, and tetronic acid analogues were synthesized to gain insights into the structural requirements for quorum sensing inhibition in Staphylococcus aureus. Compounds active against agr were noncompetitive inhibitors of the autoinducing peptide (AIP) activated AgrC receptor, by altering the activation efficacy of the cognate AIP-1. They appeared to act as negative allosteric modulators and are exemplified by 3-tetradecanoyltetronic acid 17, which reduced nasal cell colonization and arthritis in a murine infection model.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Staphylococcus aureus
/
Percepção de Quorum
/
Antibacterianos
Limite:
Animals
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article