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KMID : 0617219920030010001
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Duksung Bulletin Phamaceutical Sciences
1992 Volume.3 No. 1 p.1 ~ p.5
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The Synthesis of 1,2-Benzothiazine-3-carboxamidylhydantoin Derivatives and Antiinflammatory and Analgesic Activities
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Kwon Soon-kyoung
Park Myoung-suk
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Abstract
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A number of 4-hydroxy-2H (or alkyl)-N-(3-aralky1-2-thio-1-hydantoinyl)-1,2-benzothiazine-3-carboxamide 1,1-dioxides were synthesized through the reaction of 4-thdroxy-2H (or alkyl)-1,2-benzothiazine-3-carboxylic methyl ester 1,1-dioxide and 1-amino-2-thio-3-aralkyl-4-imidazolones in xylene. The compounds synthesized were screened for antiinflammatory effect on carrageeenin-induced edema in rat and for analgesic effect on acetic acid-induced writhing syndrome in mice. Most compounds were inhibitors of carrageenin-induced rat foot edema and some showed significant antiinflammatory activity comparable to that of indomethacin and significant analgesic activity comparable to that of indomethacin and aspirin.
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