Rofecoxib Analogues Possessing a Nitric Oxide Donor Sulfohydroxamic Acid (SO2NHOH) Cyclooxygenase-2 Pharmacophore: Synthesis, Molecular Modeling, and Biological Evaluation as Anti-inflammatory Agents

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 (N...

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Veröffentlicht in:	ChemMedChem 2012-01, Vol.7 (1), p.62-67
Hauptverfasser:	Bhardwaj, Atul, Huang, Zhangjian, Kaur, Jatinder, Knaus, Edward E.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Inflammatory Agents - chemical synthesis Anti-Inflammatory Agents - chemistry Anti-Inflammatory Agents - pharmacology biological activity Cyclooxygenase 2 - metabolism Cyclooxygenase 2 Inhibitors - chemical synthesis Cyclooxygenase 2 Inhibitors - chemistry Cyclooxygenase 2 Inhibitors - pharmacology cyclooxygenases Drug Design Humans Hydroxamic Acids - chemical synthesis Hydroxamic Acids - chemistry Hydroxamic Acids - pharmacology inflammation inhibitors Lactones - chemical synthesis Lactones - chemistry Lactones - pharmacology Male Models, Molecular Nitric Oxide - metabolism Nitric Oxide Donors - chemical synthesis Nitric Oxide Donors - chemistry Nitric Oxide Donors - pharmacology Rats Rats, Sprague-Dawley Sulfones - chemical synthesis Sulfones - chemistry Sulfones - pharmacology
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Zusammenfassung:	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.
ISSN:	1860-7179 1860-7187
DOI:	10.1002/cmdc.201100393