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目的研究烟酸衍生物的合成及其抗血小板聚集活性,为寻找新型抗血小板聚集剂提供参考。方法以烟酸为先导物,利用拼合原理,以不同的连接桥分别与乙酰水杨酸、烟酸偶联,制得目标化合物。通过体外抗血小板聚集试验对目标化合物进行抗血小板聚集活性评价。结果与结论设计合成了10个未见文献报道的烟酸衍生物,目标物的结构经ESI-MS、IR及1H-NMR谱确证。体外活性结果表明,10个目标化合物在体外均具有一定的抗血小板聚集活性,且化合物3a、3b的活性强于阳性对照药阿司匹林,值得进一步研究。
Objective To study the synthesis of nicotinic acid derivatives and its anti-platelet aggregation activity, and to provide a reference for finding a new anti-platelet aggregation agent. Methods nicotinic acid as the lead, the use of the principle of splitting, with different bridges were acetylsalicylic acid, nicotinic acid were coupled to obtain the target compound. The anti-platelet aggregation activity of the target compounds was evaluated by in vitro anti-platelet aggregation test. RESULTS AND CONCLUSION Ten non-reported nicotinic acid derivatives were designed and synthesized. The structures of the target compounds were confirmed by ESI-MS, IR and 1H-NMR. In vitro activity results showed that 10 target compounds in vitro have a certain anti-platelet aggregation activity, and compounds 3a, 3b activity is stronger than the positive control aspirin, worth further study.