4-色满酮曼尼希碱类化合物的合成及其抗血小板聚集活性  

Study on Synthesis and Anti-platelet Aggregative Activity of the Mannich Base Derivatives of 4-Chromanones

作　　者：胡春[1] 邱志远[1] 王永永[1] 肖高铿[1] 宋丽焱[1] 庞雁[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：《精细化工中间体》2010年第2期18-21,40,共5页Fine Chemical Intermediates

基　　金：国家自然科学基金资助项目(20472053)

摘　　要：4-色满酮类化合物具有广泛的生物活性。为了考察4-色满酮类化合物的抗血小板聚集活性构效关系,笔者设计合成了10种4-色满酮Mannich碱类化合物,其组成和结构经熔点、红外光谱和核磁共振氢谱确证,其中6个(5d～5g,5i～5j)目标化合物均未见文献报道。采用Born's比浊法对目标化合物进行了抗血小板聚集活性的体外筛选,实验结果表明,目标化合物对二磷酸腺苷(ADP)诱导的家兔血小板聚集均具有显著的体外抑制活性。4-Chromanones are known to exhibit a wide range of biological activities. In order to study the structure-activity relationships of anti-platelet aggregative activity of 4-chromanone derivatives,Ten Mannich bases of 4-chromanone derivatives were designed, synthesized and characterized, among which compounds （5d-5g, 5i-5j） were reported for the first time. The anti-platelet aggregative activity of the target compounds was tested using Born＇s method. Results revealed that all the target compounds showed good inhibitory activities against rabbit platelet aggregation induced by ADP in vitro.

关 键 词：4-色满酮 衍生物 合成 抗血小板聚集 

分 类 号：R914.5[医药卫生—药物化学]