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

1
Lapdesf—Laboratory of Research and Drug Development, Drugs and Medicines Department, School of Pharmaceutical Science—UNESP Rodovia Araraquara Jaú Km. 01, 14801-902, Araraquara, SP, Brazil
2
Pharmacology Laboratory, Inflammation unit, Butantan Institute, Vital Brazil Avenue 1500, 05503-900, São Paulo, Brazil
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Natural Active Principles and Toxicology Department, School of Pharmaceutical Science—UNESP Rodovia Araraquara Jaú Km. 01, 14801-902, Araraquara, SP, Brazil
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2012, 13(11), 15305-15320; https://doi.org/10.3390/ijms131115305
Received: 17 July 2012 / Revised: 17 October 2012 / Accepted: 15 November 2012 / Published: 19 November 2012
(This article belongs to the Section Biochemistry)
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. View Full-Text
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
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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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