Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect

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dos Santos, Jean Leandro ; Moreira, Vanessa ; Campos, Michel Leandro ; Chelucci, Rafael Consolin ; Barbieri, Karina Pereira ; Maggio de Castro Souto, Pollyana Cristina ; Matsubara, Marcio Hideki ; Teixeira, Catarina ; Bosquesi, Priscila Longhin ; Peccinini, Rosangela Goncalves ; Chin, Chung Man

• Tipo de documento: Artigo Científico
• Fonte: INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES; v. 13, n. 11, p. 16-pg., 2012-11-01.

Resumo

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 PGE(2) 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. (AU)

• Processo FAPESP: 10/12495-6 - Otimização, síntese e avaliação farmacológica de novos candidatos a fármacos para tratamento dos sintomas da anemia falciforme
• Beneficiário: Jean Leandro dos Santos
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 09/12664-5 - Farmacocinética pré-clínica do composto 1-(2,6-diclorofenil)indolin-2-ona (DICCIC), candidato a pró-fármaco, com propriedades anti-inflamatórias
• Beneficiário: Michel Leandro de Campos
• Modalidade de apoio: Bolsas no Brasil - Mestrado