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Keywords:

  • biological activity;
  • cyclooxygenases;
  • drug design;
  • inflammation;
  • inhibitors
Thumbnail image of graphical abstract

Expertly tailored! The development of safe anti-inflammatory (AI) agents that are highly selective COX-2 inhibitors has been challenging, as indicated by the clinical withdrawal of rofecoxib, valdecoxib, and lumiracoxib. We report novel rofecoxib analogues with a sulfohydroxamic acid nitric oxide (NO) donor COX-2 pharmacophore that exhibit potent AI activity. The release of NO is expected to circumvent the contraindicated cardiovascular effects of rofecoxib.