Enhanced water-soluble derivative of PC407 as a novel potential COX-2 inhibitor injectable formulation.
Bioorg Med Chem Lett
; 24(20): 4794-7, 2014 Oct 15.
Article
em En
| MEDLINE
| ID: mdl-25248683
ABSTRACT
PC407 is an effective COX-2 inhibitor in non-steroidal anti-inflammatory drug development but the poor solubility limits their usefulness. The aim of the study was to prepare and evaluate 4-oxo-4-[4-(5-(naphthalen-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamido]butyrate disodium, a derivative of PC407 with enhanced water solubility for injectable formulation. The prepared derivative displayed interesting high aqueous solubility (20.3 mg/mL, much superior to the parent compound PC407, 1.6 µg/mL) with confirmed in vivo analgesic activity. This derivative represents the profiles of prodrug and potential candidate of PC407 for the development of injectable COX-2 inhibitor due to extraordinary water solubility, low toxicity, and impressive analgesic activity.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirazóis
/
Sulfonamidas
/
Pró-Fármacos
/
Ciclo-Oxigenase 2
/
Inibidores de Ciclo-Oxigenase 2
Limite:
Animals
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article