Design,synthesis,and Biological Evaluation Of Phenylpropenamide Compounds As Anti-platelet Aggregationd

With the improvement of people's economic level,human health problems have shown a sub-health state.Cardiovascular and cerebrovascular diseases,according to the data show that has become one of the important factors endangering human health.According to reports,China has reached hundreds of millions of patients with cardiovascular and cerebrovascular diseases and many deaths every year millions.Thrombosis is an important factor of cardiovascular and cerebrovascular disease,platelet aggregation plays an important role in the process of angiogenesis.Therefore,it is of great research and practical significance to find anti-platelet aggregation drugs.The structure of the phenylacrylamide has been proved to be an important antiplatelet aggregation effect,while thiophene tetrahydropyridines are the parent structure of commonly used antiplatelet aggregation drugs.In this paper,with cinepazide as model compounds,20 novel phenylpropenamide compounds were designed and synthesized according to the principle of bioelectrical isotopes.The synthesized compounds were confirmed by mass spectrometry,nuclear magnetic resonance spectroscopy and infrared spectroscopy.And the anti-platelet aggregation activity test and structure-activity relationship of all the compounds were studied.Their anti-platelet aggregation activities of phenylpropenamide compounds were evaluated in vitro by bron turbidimetry.Preliminary pharmacological results showed that the compounds 6b,9b,9d and 9h have certain inhibitory effect on peanut Tetraenoic acid(AA)-induced platelet aggregation.Compounds 6b,6d,6j,9b and 9g have a certain inhibitory effect on adenosine diphosphate(ADP)-induced platelet aggregation.Compounds 6b and 9b had some inhibitory effects on AA and ADP-induced platelet aggregation,and their IC50 values respectively were 5.2 mM,5.8 mM,2.1 mM and 4.8 mM,which showed some research value.