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KMID : 0617220030140010095
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Duksung Bulletin Phamaceutical Sciences
2003 Volume.14 No. 1 p.95 ~ p.101
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COX-2 Inhibitory Activity of Hydantoin Based Derivatives
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Abstract
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For the selective candidates of COX-2 inhibitors, we designed new NSAIDs which is the hydantoin ring based structure substituted with two planar aromatic ring. Seven O-alkyl a-anilinophenylacetate were synthesized through the base-catalysis hydrolysis of 1,5-diarylhydantoins and O-alkylation of sodium a- anilinophenylacetate with alkyl halides. To evaluate inhibitory effect of COX-2. synthetic hydantoin ring based derivatives were screened with accumulation of prostaglandin by lipopolysaccharide in aspirin-treated murine macropharge cell. Most of these compounds inhibited less than 60％ of the prostaglandin E_(2) production at a concentration of 10μg/mL.
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