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

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Leblanc Y, Roy P, Boyce S, Brideau C, Chan CC, Charleson S, Gordon R, Grimm E, Guay J, Leger S, Li CS, Riendeau D, Visco D, Wang Z, Webb J, Xu LJ, Prasit P

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

Bioorg Med Chem Lett. 1999 Aug 2;9(15):2207-12.

PubMed ID

10465547 [ View in PubMed

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Abstract

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)-furanon e), a potent COX-2 inhibitor exhibiting in vivo efficacy in all models studied.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Celecoxib	Prostaglandin G/H synthase 2	IC 50 (nM)	1000	N/A	N/A	Details
Indomethacin	Prostaglandin G/H synthase 2	IC 50 (nM)	400	N/A	N/A	Details
Rofecoxib	Prostaglandin G/H synthase 2	IC 50 (nM)	500	N/A	N/A	Details