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

1,* email, 2email, 3email, 1email, 1email, 2email, 2email, 2email, 1email, 3email and 1,* email
Received: 17 July 2012; in revised form: 17 October 2012 / Accepted: 15 November 2012 / Published: 19 November 2012
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
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.
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
PDF Full-text Download PDF Full-Text [761 KB, Updated Version, uploaded 19 June 2014 04:33 CEST]
The original version is still available [743 KB, uploaded 19 June 2014 04:33 CEST]

Export to BibTeX |
EndNote


MDPI and ACS Style

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.

AMA Style

Santos JL, Moreira V, Campos ML, Chelucci RC, Barbieri KP, Souto PCMC, Matsubara MH, Teixeira C, Bosquesi PL, Peccinini RG, Chin CM. Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect. International Journal of Molecular Sciences. 2012; 13(11):15305-15320.

Chicago/Turabian Style

Santos, Jean L.; Moreira, Vanessa; Campos, Michel L.; Chelucci, Rafael C.; Barbieri, Karina P.; Souto, Pollyana C.M.C.; Matsubara, Márcio H.; Teixeira, Catarina; Bosquesi, Priscila L.; Peccinini, Rosângela G.; Chin, Chung M. 2012. "Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect." Int. J. Mol. Sci. 13, no. 11: 15305-15320.

Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert