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Rofecoxib Analogues Possessing a Nitric Oxide Donor Sulfohydroxamic Acid (SO 2 NHOH) Cyclooxygenase‐2 Pharmacophore: Synthesis, Molecular Modeling, and Biological Evaluation as Anti‐inflammatory Agents
Author(s) -
Bhardwaj Atul,
Huang Zhangjian,
Kaur Jatinder,
Knaus Edward E.
Publication year - 2012
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100393
Subject(s) - rofecoxib , pharmacophore , valdecoxib , nitric oxide , cyclooxygenase , chemistry , pharmacology , prostaglandin endoperoxide synthase , medicine , combinatorial chemistry , stereochemistry , enzyme , biochemistry , organic chemistry
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.