Racemic and chiral sulfoxides as potential prodrugs of the COX-2 inhibitors Vioxx and Arcoxia.
Bioorg Med Chem Lett
; 16(12): 3209-12, 2006 Jun 15.
Article
en En
| MEDLINE
| ID: mdl-16616494
ABSTRACT
The preparation of the sulfoxide analogues 2 and 4, and their enantiomeric pure forms is discussed as well as their potential to act as prodrugs to the potent and selective sulfone-containing COX-2 inhibitors rofecoxib and etoricoxib. Sulfoxides 2 and 4 were shown to be effectively transformed in vivo into rofecoxib and etoricoxib, respectively, after oral administration in rats. In the case of sulfoxide 2, both a slightly improved pharmacokinetic profile and a better pharmacological activity in an arthritis model were seen when compared with rofecoxib.
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Banco de datos:
MEDLINE
Asunto principal:
Piridinas
/
Safrol
/
Sulfonas
/
Profármacos
/
Inhibidores de la Ciclooxigenasa 2
/
Lactonas
Límite:
Animals
/
Humans
/
Male
Idioma:
En
Año:
2006
Tipo del documento:
Article