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. Detailed facts of importance to specialist readers are published as "Supporting Information". Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
Keywords
RofecoxibPharmacophoreValdecoxibNitric oxideCyclooxygenaseChemistryPharmacologyProstaglandin-Endoperoxide SynthaseMedicineCombinatorial chemistryStereochemistryEnzymeBiochemistryOrganic chemistry
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Publication Info
- Year
- 2011
- Type
- article
- Volume
- 7
- Issue
- 1
- Pages
- 62-67
- Citations
- 27
- Access
- Closed
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Cite This
Atul Bhardwaj,
Zhangjian Huang,
Jatinder Kaur
et al.
(2011).
Rofecoxib Analogues Possessing a Nitric Oxide Donor Sulfohydroxamic Acid (SO<sub>2</sub>NHOH) Cyclooxygenase‐2 Pharmacophore: Synthesis, Molecular Modeling, and Biological Evaluation as Anti‐inflammatory Agents.
ChemMedChem
, 7
(1)
, 62-67.
https://doi.org/10.1002/cmdc.201100393
Identifiers
- DOI
- 10.1002/cmdc.201100393