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

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Li CS, Black WC, Brideau C, Chan CC, Charleson S, Cromlish WA, Claveau D, Gauthier JY, Gordon R, Greig G, Grimm E, Guay J, Lau CK, Riendeau D, Therien M, Visco DM, Wong E, Xu L, Prasit P

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

Bioorg Med Chem Lett. 1999 Nov 15;9(22):3181-6.

PubMed ID
10576684 [ View in PubMed
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Abstract

By inserting an oxygen link between the 3-fluorophenyl and the lactone ring of 5,5-dimethyl-3-(3fluorophenyl)-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.

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