YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

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

Benzothiazine-3-carboxamide 유도체의 합성과 COX-2 저해효과

  • 신혜순 (덕성여자대학교 약학대학) ;
  • 최희전 (덕성여자대학교 약학대학) ;
  • 권순경 (덕성여자대학교 약학대학)
  • Published : 2002.12.01
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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

References

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