MexAB-OprM-specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 1: discovery and early strategies for lead optimization.
Bioorg Med Chem Lett
; 13(23): 4201-4, 2003 Dec 01.
Article
em En
| MEDLINE
| ID: mdl-14623001
ABSTRACT
The identification of a series of compounds that specifically inhibit efflux by the MexAB-OprM pump system in Pseudomonas aeruginosa is described. Synthesis and in vitro structure-activity relationships (SARs) are outlined. Early leads lacked activity in animal models, and efforts to improve solubility and reduce serum protein binding by the introduction of polar groups are discussed.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Proteínas de Membrana Transportadoras
/
Pseudomonas aeruginosa
/
Proteínas da Membrana Bacteriana Externa
/
Transporte Biológico Ativo
/
Proteínas de Transporte
/
Antibacterianos
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2003
Tipo de documento:
Article
País de afiliação:
Japão