약학회지 (YAKHAK HOEJI)

  • 제46권6호
  • /
  • Pages.375-380
  • /
  • 2002
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  • 0377-9556(pISSN)
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  • 2383-9457(eISSN)
대한약학회 (The Pharmaceutical Society of Korea)
권호 표지

Benzothiazine-3-carboxamide 유도체의 합성과 COX-2 저해효과

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

  • 신혜순 (덕성여자대학교 약학대학) ;
  • 최희전 (덕성여자대학교 약학대학) ;
  • 권순경 (덕성여자대학교 약학대학)
  • 발행 : 2002.12.01
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초록

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.

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참고문헌

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