A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors

By inserting an oxygen link between the 3-fluorophenyl and the lactone ring of 5,5-dimethyl-3-(3-fluorophenyl)-4-(4-methanesulfonylphenyl)-2(5H)-furanone 1 (DFU), analogs with enhanced in vitro COX-2 inhibitory potency as well as in vivo potency in models of inflammation were obtained. By inserting...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-11, Vol.9 (22), p.3181-3186
Hauptverfasser:	Li, Chun-Sing, Black, W.Cameron, Brideau, Christine, Chi Chung Chan, Charleson, Stella, Cromlish, Wanda A., Claveau, David, Gauthier, Jacques Yves, Gordon, Robert, Greig, Gillian, Grimm, Erich, Guay, Jocelyne, Lau, Cheuk K., Riendeau, Denis, Thérien, Michel, Visco, Denise M., Wong, Elizabeth, Lijing Xu, Prasit, Petpiboon
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacology Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents CHO Cells Cricetinae Cyclooxygenase 2 Cyclooxygenase 2 Inhibitors Cyclooxygenase Inhibitors - chemistry Cyclooxygenase Inhibitors - pharmacokinetics Cyclooxygenase Inhibitors - pharmacology Furans - chemistry Furans - pharmacokinetics Furans - pharmacology Isoenzymes - drug effects Medical sciences Pharmacology. Drug treatments Prostaglandin-Endoperoxide Synthases - drug effects Rats Structure-Activity Relationship
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Zusammenfassung:	By inserting an oxygen link between the 3-fluorophenyl and the lactone ring of 5,5-dimethyl-3-(3-fluorophenyl)-4-(4-methanesulfonylphenyl)-2(5H)-furanone 1 (DFU), analogs with enhanced in vitro COX-2 inhibitory potency as well as in vivo potency in models of inflammation were obtained. By inserting an oxygen link between the aryl group and the lactone ring, analogs with enhanced COX-2 and antiinflammatory activity could be obtained.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00559-4