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Synthesis and COX-2 Inhibitory Activity of Benzothiazine-3-carboxamide Derivatives  

신혜순 (덕성여자대학교 약학대학)
최희전 (덕성여자대학교 약학대학)
권순경 (덕성여자대학교 약학대학)
Publication Information
YAKHAK HOEJI / v.46, no.6, 2002 , pp. 375-380 More about this Journal
Abstract
In this study, newly designed COX-2 inhibitors, synthetic derivatives of benzothiazine-3-carboxamide, were screened in vitro for selectivity of COX-1 and COX-2 inhibition properties. 7-Bromo-1,2-benzoisothiazine derivatives were obtained from 4-bromotoluene over the chlorosulfonation, amination and oxidation. And benzothiazine ring was synthesized through Gabriel-Colmann rearrangement reaction. To evaluate inhibitory effect of COX-2, synthetic derivatives of benzothiazine-3-carboxamide were tested with accumulation of prostaglandin by lipopolysaccharide in aspirin-treated murine macropharge cell. Some of the synthesized lead compounds have potentially shown the structure-activity relationship for selectivity of COX-2 inhibition activity.
Keywords
benzothiazine-3-carboxamide derivatives; cyclooxygenase-2 inhibitor;
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