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Int. J. Mol. Sci. 2012, 13(12), 17244-17274; doi:10.3390/ijms131217244
Review

Prodrugs of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs), More Than Meets the Eye: A Critical Review

1,2
Received: 13 July 2012; in revised form: 29 November 2012 / Accepted: 10 December 2012 / Published: 17 December 2012
(This article belongs to the Section Bioactives and Nutraceuticals)
Abstract: The design and the synthesis of prodrugs for nonsteroidal anti-inflammatory drugs (NSAIDs) have been given much attention by medicinal chemists, especially in the last decade. As a therapeutic group, NSAIDs are among the most widely used prescribed and over the counter (OTC) medications. The rich literature about potential NSAID prodrugs clearly shows a shift from alkyl, aryalkyl or aryl esters with the sole role of masking the carboxylic acid group, to more elaborate conjugates that contain carefully chosen groups to serve specific purposes, such as enhancement of water solubility and dissolution, nitric oxide release, hydrogen sulfide release, antioxidant activity, anticholinergic and acetylcholinesterase inhibitory (AChEI) activity and site-specific targeting and delivery. This review will focus on NSAID prodrugs that have been designed or were, later, found to possess intrinsic pharmacological activity as an intact chemical entity. Such intrinsic activity might augment the anti-inflammatory activity of the NSAID, reduce its side effects or transform the potential therapeutic use from classical anti-inflammatory action to something else. Reports discussed in this review will be those of NO-NSAIDs, anticholinergic and AChEI-NSAIDs, Phospho-NSAIDs and some miscellaneous agents. In most cases, this review will cover literature dealing with these NSAID prodrugs from the year 2006 and later. Older literature will be used when necessary, e.g., to explain the chemical and biological mechanisms of action.
Keywords: anti-inflammatory; cyclooxygenase; codrug; mutual prodrug; NO-NSAIDs; NSAIDs; Phospho-NSAIDs; prodrug anti-inflammatory; cyclooxygenase; codrug; mutual prodrug; NO-NSAIDs; NSAIDs; Phospho-NSAIDs; prodrug
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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MDPI and ACS Style

Qandil, A.M. Prodrugs of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs), More Than Meets the Eye: A Critical Review. Int. J. Mol. Sci. 2012, 13, 17244-17274.

AMA Style

Qandil AM. Prodrugs of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs), More Than Meets the Eye: A Critical Review. International Journal of Molecular Sciences. 2012; 13(12):17244-17274.

Chicago/Turabian Style

Qandil, Amjad M. 2012. "Prodrugs of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs), More Than Meets the Eye: A Critical Review." Int. J. Mol. Sci. 13, no. 12: 17244-17274.



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