6-[4-(取代胺基乙酰胺基苯基)]-4,5-二氢-3(2H)哒嗪酮类化合物的合成及其抗血小板聚集活性研究  

Synthesis and antiplatelet aggregative activity of 6-[4-(substituted amino acetamido-phenyl)]-4,5-dihydro-3(2H)-pyridazinones

作　　者：柴晓云[1] 张晨曦[2] 胡宏岗[1] 赵庆杰[1] 但志刚[1] 邹燕[1] 俞世冲[1] 吴秋业[1] 

机构地区：[1]第二军医大学药学院有机化学教研室,上海200433 [2]中国人民解放军第305医院,北京100017

出　　处：《药学实践杂志》2008年第6期444-446,467,共4页Journal of Pharmaceutical Practice

基　　金：上海市长宁区科委科研项目(20054Y17001);上海市重点学科资助项目(B906).

摘　　要：目的：合成新的含有胺基的哒嗪酮类化合物，并研究其对抗血小板聚集活性的影响。方法：以乙酰基为连接片段，引入不同的取代胺基，设计合成未见报道的目标化合物8个，所有化合物均经过。H—NMR谱等确证；体外药理实验参考Born方法进行。结果：所有化合物都具有体外抑制血小板聚集的活性，其中化合物（1），（3）和（8）的活性较强，化合物（3）的活性是MCI-154的6倍。结论：引入不同的取代胺基，对化合物抑制血小板聚集的活性有影响。Objective： To synthesize new pyridazinone derivatives substituted by different amino groups. Methods： Eight target compounds were designed and synthesized by inletting different substituted amino groups connecting through the acetyl fragment. All of them were confirmed by ^1H-NMR spectra. Born method was applied for preliminary pharmacological test in vitro. Results ： All of the target compounds were reported for the first time. The results of preliminary pharmacological test showed that all the target compounds exhibited potent antiplatelet aggregative activity to a certain extent. Compounds （ 1 ）, （3） and （8） have better activeties; compound （3） showed a 6 times higher activity than that of MCI-154. Condusion：Inletting different substituted amino groups can enhance the antiplatelet aggregation activity of the compounds.

关 键 词：化学合成 哒嗪酮类 体外抗血小板聚集活性 

分 类 号：R914.5[医药卫生—药物化学]