4-苯甲酰胺基苯磺酰胺类化合物的合成及其抗炎活性  

Studies on the synthesis and antiinflammatory activity of 4-benzamidobenzenesulfonamide derivatives

作　　者：楼永军[1] 邓海霞[1] 董金华[1] 计志忠[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2003年第6期339-341,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计并合成 4 苯甲酰胺基苯磺酰胺类化合物 ,研究其抗炎活性和构效关系。方法以取代苯甲酸为原料合成目标化合物 ,并以二甲苯致小鼠耳肿胀模型测试目标化合物的抗炎活性。结果共合成 7个化合物 (其中 6个化合物未见CA报道 ) ,经红外光谱、核磁共振氢谱和质谱确证其结构 ,部分化合物对二甲苯致耳肿胀具有较强的抑制作用 ,并初步总结了构效关系。结论 4 苯甲酰胺基苯磺酰胺类化合物具有较强的抗炎活性。Aim To design and synthesize 4 benzamidobenzenesulfonamide derivatives and study their antiinflammatory activity and structure activity relationship.Methods The target compounds were synthesized from substituted benzoic acids via three steps and were evaluated with the model of xylene induced ear edema in mice.Results Seven compounds were obtained and confirmed by the spectral detection.Some compounds exerted significant antiinflammatory activity and their structure activity relationships were stated preliminarily.Conclusion 4 Benzamidobenzenesulfonamide derivatives have appreciable antiinflammatory activity.

关 键 词：药物化学 构效关系 化学合成 4-苯甲酰胺基苯磺酰胺 抗炎活性 

分 类 号：R914[医药卫生—药物化学]