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KMID : 0370220040480020141
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Yakhak Hoeji
2004 Volume.48 No. 2 p.141 ~ p.146
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Synthesis and Screening of Cyclooxygenase Activity of Hydantoin and 2-Thiohydantoin Derivatives
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신혜순/Shin HS
최희전/권순경/Choi HJ/Kwon SK
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Abstract
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Selective COX-2 inhibitors were expected to retain anti-inflammatory activity by inhibition of prostaglandin production with reduction of gastric and renal side effect associa ted 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 hererocyclic ring substituted with two aryl groups, phenol 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 IC50 = 13.13 ~ 18.78 ㎍/ml for the development of COX-2 inhibitors.
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KEYWORD
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