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Pharmaceuticals 2010, 3(5), 1530-1549; doi:10.3390/ph3051530

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): Progress in Small Molecule Drug Development

* ,  and
School of Pharmacy, Health Sciences Campus, University of Waterloo, 200 University Avenue W. Waterloo, ON, N2L 3G1 Canada
* Author to whom correspondence should be addressed.
Received: 1 April 2010 / Revised: 22 April 2010 / Accepted: 12 May 2010 / Published: 14 May 2010
(This article belongs to the collection Non-Steroidal Anti-Inflammatory Drugs)


Ever since the discovery of aspirin, small molecule therapeutics have been widely prescribed to treat inflammation and pain. Aspirin and several small molecule NSAIDs are known to inhibit the enzymes cyclooxygenase-1 (COX-1) and -2 (COX-2). Despite the success of NSAIDs to treat inflammatory disorders, the development of a clinically useful small molecule NSAIDs with decreased side effect profiles is an ongoing effort. The recent discovery and development of selective COX-2 inhibitors was a step toward this direction. Emerging trends are represented by the progress in the development of hybrid agents such as nitric oxide donor-NSAIDs (NO-NSAIDs) and dual COX/lipoxygenase (LOX) inhibitors. This review focuses on the recent advances in the rational design of small molecule NSAIDs in therapy.
Keywords: Small molecules; NSAIDs; Lp-PLA2; mPGES-1; TNF-α Small molecules; NSAIDs; Lp-PLA2; mPGES-1; TNF-α
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Rao, P.P.N.; Kabir, S.N.; Mohamed, T. Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): Progress in Small Molecule Drug Development. Pharmaceuticals 2010, 3, 1530-1549.

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