SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor

Extensive SAR has been established in the alkoxy lactone series and this has lead to the discovery of DFP (5,5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanone), a potent COX-2 inhibitor exhibiting in vivo efficacy in all models studied. DFP was found to be a potent and highly selectiv...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-08, Vol.9 (15), p.2207-2212
Hauptverfasser:	Leblanc, Y., Roy, P., Boyce, S., Brideau, C., Chan, C.C., Charleson, S., Gordon, R., Grimm, E., Guay, J., Léger, S., Li, C.S., Riendeau, D., Visco, D., Wang, Z., Webb, J., Xu, L.J., Prasit, P.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cyclooxygenase 2 Cyclooxygenase 2 Inhibitors Cyclooxygenase Inhibitors - chemical synthesis Cyclooxygenase Inhibitors - chemistry Cyclooxygenase Inhibitors - pharmacokinetics Cyclooxygenase Inhibitors - pharmacology Humans Isoenzymes - drug effects Isoenzymes - metabolism Macaca mulatta Medical sciences Membrane Proteins Pharmacology. Drug treatments Prostaglandin-Endoperoxide Synthases - drug effects Prostaglandin-Endoperoxide Synthases - metabolism Rats Saimiri Structure-Activity Relationship U937 Cells
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Zusammenfassung:	Extensive SAR has been established in the alkoxy lactone series and this has lead to the discovery of DFP (5,5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanone), a potent COX-2 inhibitor exhibiting in vivo efficacy in all models studied. DFP was found to be a potent and highly selective COX-2 inhibitor.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00365-0