%0 Journal Article
%T Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
%A Jean Leandro dos Santos
%A Vanessa Moreira
%A Michel Leandro Campos
%A Rafael Consolin Chelucci
%A Karina Pereira Barbieri
%A Pollyana Cristina Maggio de Castro Souto
%A M¨˘rcio Hideki Matsubara
%A Catarina Teixeira
%A Priscila Longhin Bosquesi
%A Rosangela Gon£żalves Peccinini
%A Chung Man Chin
%J International Journal of Molecular Sciences
%D 2012
%I MDPI AG
%R 10.3390/ijms131115305
%X 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.
%K NSAIDs
%K anti-inflammatory
%K diclofenac
%K prodrugs
%K molecular modification
%K lactam
%K COX-inhibitor
%K bioconversion
%K chronic inflammation
%U http://www.mdpi.com/1422-0067/13/11/15305