Immobilization of a novel antibacterial agent on solid phase and subsequent isolation of EF-Tu.
Bioconjug Chem
; 15(2): 333-43, 2004.
Article
en En
| MEDLINE
| ID: mdl-15025529
Screening of our compound collection identified PNU-92560, a 2-[1,3,4]thiadiazolo[3,2-a]pyrimidine-6-carboxamide, as a novel antibacterial agent. Extensive analogue development identified that the 2-position of the thiadiazole could be functionalized with a linker that would allow the compound to be attached to a solid support. The extreme insolubility of the analogues prevented the mechanism of action for these compounds to be determined utilizing traditional methodology. The solid-supported compounds were utilized as affinity columns to identify elongation factor Tu (EF-Tu) as a putative target for this class of compounds. The activity of the compounds in a metabolic labeling experiments and in translation assay supports the identity of the target for these compounds to be EF-Tu.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirimidinas
/
Tiazoles
/
Factor Tu de Elongación Peptídica
/
Antibacterianos
Tipo de estudio:
Prognostic_studies
Idioma:
En
Revista:
Bioconjug Chem
Asunto de la revista:
BIOQUIMICA
Año:
2004
Tipo del documento:
Article
País de afiliación:
Estados Unidos
Pais de publicación:
Estados Unidos