Benzothiazine-3-carboxamide 유도체의 합성과 CGX-2 저해효과

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

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.