Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.

Article Details

Citation

Lau CK, Brideau C, Chan CC, Charleson S, Cromlish WA, Ethier D, Gauthier JY, Gordon R, Guay J, Kargman S, Li CS, Prasit P, Riendeau D, Therien M, Visco DM, Xu L

Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.

Bioorg Med Chem Lett. 1999 Nov 15;9(22):3187-92.

PubMed ID
10576685 [ View in PubMed
]
Abstract

A series of 3-heteroaryloxy4-phenyl-2-5H)-furanones were prepared and evaluated for their potency and selectivity as COX-2 inhibitors. This led to the identification of L-778,736 as a potent, orally active and selective inhibitor of the COX-2 enzyme.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
CelecoxibProstaglandin G/H synthase 2IC 50 (nM)2N/AN/ADetails
CelecoxibProstaglandin G/H synthase 2IC 50 (nM)1000N/AN/ADetails
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)500N/AN/ADetails
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)26N/AN/ADetails
RofecoxibProstaglandin G/H synthase 2IC 50 (nM)20N/AN/ADetails
RofecoxibProstaglandin G/H synthase 2IC 50 (nM)500N/AN/ADetails