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Int. J. Mol. Sci. 2012, 13(11), 15305-15320; doi:10.3390/ijms131115305
Article

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

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Received: 17 July 2012 / Revised: 17 October 2012 / Accepted: 15 November 2012 / Published: 19 November 2012
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
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Abstract

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.
Keywords: NSAIDs; anti-inflammatory; diclofenac; prodrugs; molecular modification; lactam; COX-inhibitor; bioconversion, chronic inflammation NSAIDs; anti-inflammatory; diclofenac; prodrugs; molecular modification; lactam; COX-inhibitor; bioconversion, chronic inflammation
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Santos, J.L.; Moreira, V.; Campos, M.L.; Chelucci, R.C.; Barbieri, K.P.; Souto, P.C.M.C.; Matsubara, M.H.; Teixeira, C.; Bosquesi, P.L.; Peccinini, R.G.; Chin, C.M. Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect. Int. J. Mol. Sci. 2012, 13, 15305-15320.

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