New celecoxib derivatives as anti-inflammatory agents.

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Szabo G, Fischer J, Kis-Varga A, Gyires K

New celecoxib derivatives as anti-inflammatory agents.

J Med Chem. 2008 Jan 10;51(1):142-7. Epub 2007 Dec 12.

PubMed ID

18072726 [ View in PubMed

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Abstract

A series of 1,5-diarylpyrazoles with a substituted benzenesulfonamide moiety was synthesized and evaluated for cyclooxygenase (COX-1/COX-2) inhibitory activities. Some compounds, for example, (+/-)-2-[4-(5- p-tolyl-3-trifluoromethyl-pyrazole-1-yl)-benzenesulfonylaminooxy]-propionic acid 16 and its disodium salt 21, had a higher in vivo anti-inflammatory activity compared to celecoxib, despite having no in vitro COX-1 or COX-2 inhibitory activity. Their gastrointestinal side effect profile is essentially more favorable than that of celecoxib.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Valdecoxib	Prostaglandin G/H synthase 2	IC 50 (nM)	40	N/A	N/A	Details