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NO供体型烟酸衍生物的合成及其生物活性研究
引用本文:汪电雷,吴亚先,陈维珍,何黎琴,王效山.NO供体型烟酸衍生物的合成及其生物活性研究[J].化学世界,2013,54(3):165-168.
作者姓名:汪电雷  吴亚先  陈维珍  何黎琴  王效山
作者单位:安徽中医学院药学院,安徽省现代中药重点实验室,安徽合肥230031
基金项目:安徽省教育厅自然科学重点研究项目
摘    要:为寻找活性更强、副作用更小的烟酸前体药物,以烟酸为先导物,设计、合成了5个硝酸酯类NO供体型烟酸衍生物。经红外光谱、核磁共振氢谱及质谱确证了该目标化合物的化学结构。通过体外抗血小板聚集试验、及体内调血脂作用对目标化合物进行生物活性评价。结果表明目标化合物具有较强的体外抗血小板聚集活性及体内良好的降脂作用。

关 键 词:烟酸  硝酸酯  NO供体  抗血小板聚集  调脂作用

Synthesis and Biological Evaluation of Nitric Oxide Releasing Nicotinic Acid Derivatives
WANG Dian-lei,WU Ya-xian,CHEN Wei-zhen,HE Li-qin,WANG Xiao-shan.Synthesis and Biological Evaluation of Nitric Oxide Releasing Nicotinic Acid Derivatives[J].Chemical World,2013,54(3):165-168.
Authors:WANG Dian-lei  WU Ya-xian  CHEN Wei-zhen  HE Li-qin  WANG Xiao-shan
Affiliation:(Anhui College of Traditional Chinese Medicine,Anhui Key Laboratory of Modernized Chinese Material Medical,Auhui Hefei 230031,China)
Abstract:To screen out nicotinic acid prodrugs with better activity and less side effects,five nicotinic acid derivatives conjugated with nitric oxide(NO) donor were designed and synthesized from nicotinic acid as leading compound.Their structures were characterized by IR,MS and 1H NMR spectroscopy.Anti-platelet aggregation and lipidemic-modulating activities of the target compounds were evaluated.It was found that all of the synthesized compounds possessed good anti-platelet aggregation and lipidemic-modulating action.
Keywords:nicotinic acid  nitrate  NO donor  anti-platelet aggregation  lipidemic-modulating activities
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