Development of a triclosan scaffold which allows for adaptations on both the A- and B-ring for transport peptides.
Bioorg Med Chem Lett
; 23(12): 3551-5, 2013 Jun 15.
Article
em En
| MEDLINE
| ID: mdl-23664871
The enoyl acyl-carrier protein reductase (ENR) enzyme is harbored within the apicoplast of apicomplexan parasites providing a significant challenge for drug delivery, which may be overcome through the addition of transductive peptides, which facilitates crossing the apicoplast membranes. The binding site of triclosan, a potent ENR inhibitor, is occluded from the solvent making the attachment of these linkers challenging. Herein, we have produced 3 new triclosan analogs with bulky A- and B-ring motifs, which protrude into the solvent allowing for the future attachment of molecular transporters for delivery.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Triclosan
/
Proteínas de Transporte
/
Enoil-(Proteína de Transporte de Acila) Redutase (NADH)
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article