The search for new COX-2 inhibitors: a review of 2002 – 2008 patents

Abstract

Background: Two COX isoenzymes are known, COX-1 and COX-2, for which the main inhibitors are the NSAIDs. The common anti-inflammatory drugs (such as aspirin, ibuprofen and naproxen) all act by blocking the action of both the COX-1 and COX-2 enzymes. The COX-2 inhibitors represent a new class of drugs that do not affect COX-1 but selectively block COX-2. This selective action provides the benefits of reducing inflammation without irritating the stomach and cardiovascular effects. Objective: This review focuses on patents published in the field during 2002 – 2008, paying particular attention to promising COX-2 inhibitors. Conclusion: Structural analogues of the COX-2 inhibitors celecoxib and valdecoxib, and novel potential pyridazine, triazole, indole and thione derivatives emerge as promising leads for the treatment of inflammation, pain and other diseases.

Keywords::

• anti-inflammatory drugs
• COX-2
• NSAIDs
• patents

Acknowledgement

The authors thank the Brazilian agencies Fundação de Amparo à Pesquisa do Estado de Minas Gerais and Conselho Nacional de Desenvolvimento Científico e Tecnológico for funding part of this work.

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