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Synthesis and Screening of Cyclooxygenase Activity of Hydantoin and 2-Thiohydantoin Derivatives  

신혜순 (덕성여자대학교 약학대학)
최희전 (덕성여자대학교 약학대학)
권순경 (덕성여자대학교 약학대학)
Publication Information
YAKHAK HOEJI / v.48, no.2, 2004 , pp. 141-146 More about this Journal
Abstract
Selective COX-2 inhibitors were expected to retain anti-inflammatory activity by inhibition of prostaglandin production with reduction of gastric and renal side effect associated with non-steroidal anti-inflammatory drugs. This study reported the syntheses of novel 2-thiohydantoin and hydantoin derivatives which have the structure of 5-membered heterocyclic ring substituted with two aryl groups, phenyl group at 5-position and p-sulfamylphenyl or p-methoxyphenyl group at 1-position. These synthetic compounds showed significant COX-2 activities in vitro screening. Among them, 5-phenyl-2-thiohydantoin and hydantoin substituted with benzyl group at 3-position, compounds 5 and 8, could be considered as lead compounds with $IC_{50}$/=13.13∼18.78 $\mu\textrm{g}$/$m\ell$ for the development of COX-2 inhibitors.
Keywords
2-thiohydantoin and hydantoin derivatives; cyclooxygenase-2 inhibitor;
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