7-甲磺酰胺基-6-苯氧基-4-色满酮衍生物的合成及抗炎活性研究  

Studies on the synthesis and antiinflammatoryactivity of novel 7-methanesulfonylamino-6-phenoxy-chromanone derivatives

作　　者：高河勇[1] 王丽[1] 徐莉英[1] 董金华[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5期260-263,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计合成7-甲磺酰胺基-6-苯氧基-4-色满酮衍生物,并研究其抗炎活性。方法以4-氨基-3-硝基苯甲醚、芳香醛等为原料,经多步反应合成目标化合物。以二甲苯致小鼠耳肿胀炎症模型筛选所合成化合物的抗炎活性。结果共合成9个未见CA报道的化合物,经1H-MNR、IR和MS确证其结构,其中有3个化合物在200 mg/kg的剂量下,活性好于10 mg/kg剂量的吲哚美辛(indomethacin),4个化合物的活性略低于10 mg/kg剂量下的吲哚美辛。结论部分7-甲磺酰胺基-6-苯氧基-4-色满酮的3位取代芳基亚甲基类化合物有较强的抗炎活性,活性与芳香环的结构密切相关。Aim To design and synthesize the novel 7-methanesulfonylamino-6-phenoxy-chromanone derivatives, and to evaluate their antiinflammatory activities. Methods The target compounds were synthesized from 4-amino-3-nitroanisole, aromatic aldehyde and other chemicals via a nine step reaction, and their inhibitory effects on xylene-induced ear edema in mice were screened. Results Nine new compounds were synthesized and identified by 1H-NMR, IR, MS. The antiinflammatory effects of the three compounds at the dosage of 200 mg/kg were equal or superior to that of indomethacin at the dosage of 10 mg/kg, and four compounds at the dosage of 200 mg/kg were a bit less potent than indomethacin at the dosage of 10 mg/kg. Conclusions Some 7-methanesulfonylamino-6-phenoxy-3-substituted arylmethylidene-chromanones exerted very potent antiinflammatory activities. There is apparent relationship between the structure of the aryl ring of 3-arylmethylidene of the target compounds and the bioactivities.

关 键 词：药物化学 制备 化学合成 色满酮衍生物 抗炎 

分 类 号：R914[医药卫生—药物化学]