Cyclooxygenase-2 inhibitors: a literature and patent review (2009 - 2010)

Expert Opin Ther Pat. 2011 Sep;21(9):1339-432. doi: 10.1517/13543776.2011.593510. Epub 2011 Jun 29.


Introduction: COXs catalyze the complex conversion of arachidonic acid to prostaglandins and thromboxanes, which trigger as autacoids with autocrine and paracrine biological effects many physiological and pathophysiological responses. The structural similarities of the COX-1 and -2 enzymes make the search for selective inhibitors for COX-2 versus -1 a formidable challenge.

Areas covered: The present review provides a survey of the development of novel COX-2 inhibitors covering literature and patents between 2009 and 2010. The presence of a central, typically 1,2-diaryl substituted, heterocycle or carbocycle as a characteristic structural motif in many selective COX-2 inhibitors represents the basis of their classification in this review. The classification in this review includes COX-2 inhibitors based on five- and six-membered heterocycles, benzoheterocycles (e.g., benzopyrans, benzopyranones, indoles and quinolines), quinones, chalcones, natural products and miscellaneous. When available, COX-2 inhibitors are presented with their related COX-2 inhibitory potency and selectivity.

Expert opinion: The availability of detailed information on the crystal structure of the COX-2 enzyme with various substrates, cofactors and inhibitors, and the recently reported increased risk of cardiovascular events associated with selective COX-2 inhibitors will further stimulate development of COX-2 inhibitors with favorable COX-2 inhibition profiles without adverse effects to the cardiovascular system.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Biological Products / pharmacology
  • Cyclooxygenase 1 / metabolism
  • Cyclooxygenase 2 Inhibitors / chemical synthesis*
  • Cyclooxygenase 2 Inhibitors / pharmacology*
  • Cyclooxygenase Inhibitors / chemical synthesis
  • Cyclooxygenase Inhibitors / pharmacology
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / pharmacology
  • Humans
  • Mice
  • Patents as Topic
  • Structure-Activity Relationship
  • Substrate Specificity


  • Anti-Inflammatory Agents, Non-Steroidal
  • Biological Products
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Heterocyclic Compounds
  • Cyclooxygenase 1