Design, synthesis, and evaluation of oxazole transthyretin amyloidogenesis inhibitors.
Bioorg Med Chem Lett
; 15(4): 1075-8, 2005 Feb 15.
Article
en En
| MEDLINE
| ID: mdl-15686915
ABSTRACT
Ten oxazoles bearing a C(4) carboxyl group were synthesized and evaluated as transthyretin (TTR) amyloid fibril inhibitors. Substituting aryls at the C(2) position of the oxazole ring reveals that a 3,5-dichlorophenyl substituent significantly reduced amyloidogenesis. The efficacy of these inhibitors was enhanced further by installing an ethyl, a propyl, or a CF(3) group at the C(5) position. The CF(3) substitution at C(5) also improves the TTR binding selectivity over all the other proteins in human blood.
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Bases de datos:
MEDLINE
Asunto principal:
Oxazoles
/
Prealbúmina
/
Amiloide
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2005
Tipo del documento:
Article
País de afiliación:
Estados Unidos