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Dr. Atul Bhardwaj, Dr. Zhangjian Huang, Dr. Jatinder Kaur and Prof. Edward E. Knaus Rofecoxib Analogues Possessing a Nitric Oxide Donor Sulfohydroxamic Acid (SO2NHOH) Cyclooxygenase-2 Pharmacophore: Synthesis, Molecular Modeling, and Biological Evaluation as Anti-inflammatory Agents ChemMedChem 7

Article first published online: 11 OCT 2011 | DOI: 10.1002/cmdc.201100393

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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.

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