Benzothiazine-3-carboxamide 유도체의 합성과 CGX-2 저해효과

• 영문명: Synthesis and COX-2 Inhibitory Activity of Benzothlazine-3-carboxamide Derivatives
• 발행기관: 대한약학회
• 저자명: 신혜순(Hea Soon Shin) 최희전(Hee Jeon Choi) 권순경(Soon Kyoung Kwon)
• 간행물 정보: 『약학회지』제46권 제6호 (2002년), 375~380쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2002.12.31

영문 초록

In tai s study, newly de signed 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 erect 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.

키워드

benzothiazine-3-carboxamide derivatives cyclooxygenase-2 inhibitor.