| Autor: |
Santos, Jean Leandro dos, Moreira, Vanessa, Campos, Michel Leandro, Chelucci, Rafael Consolin, Barbieri, Karina Pereira, de Castro Souto, Pollyana Cristina Maggio, Matsubara, Márcio Hideki, Teixeira, Catarina, Bosquesi, Priscila Longhin, Peccinini, Rosângela Gonçalves, Chung Man Chin |
| Předmět: |
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| Zdroj: |
International Journal of Molecular Sciences; Nov2012, Vol. 13 Issue 11, p15305-15320, 16p, 1 Diagram, 1 Chart, 5 Graphs |
| Abstrakt: |
Long-term nonsteroidal anti-inflammatory drugs (NSAIDs) therapy has been associated with several adverse effects such as gastric ulceration and cardiovascular events. Among the molecular modifications strategies, the prodrug approach is a useful tool to discover new safe NSAIDs. The 1-(2,6-dichlorophenyl)indolin-2-one is a diclofenac prodrug which demonstrated relevant anti-inflammatory properties without gastro ulceration effect. In addition, the prodrug decreases PGE2 levels, COX-2 expression and cellular influx into peritoneal cavity induced by carrageenan treatment. Preliminary pharmacokinetic studies have shown in vivo bioconversion of prodrug to diclofenac. This prodrug is a new nonulcerogenic NSAID useful to treat inflammatory events by long-term therapy. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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