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依据拼合原理,设计并合成了20个具有苯丙烯酰胺类结构的化合物,其结构均经IR、~1H NMR、~(13)C NMR和MS确证。采用Bron比浊法测定了所有化合物对二磷酸腺苷(adenosine diphoshate,ADP)及花生四烯酸(arachidonic acid,AA)诱导的血小板聚集的抑制活性。初步药理结果显示,化合物6b、9b、9d和9h对AA诱导的血小板聚集具有较好的抑制作用;化合物6b、6d、6j、9b和9g对ADP诱导的血小板聚集具有较好的抑制作用。
According to the principle of assembly, 20 compounds with phenyl acrylamide structure were designed and synthesized. Their structures were confirmed by IR, 1H NMR, 13 C NMR and MS. All compounds were tested for their inhibitory activity against platelet aggregation induced by adenosine diphoshate (ADP) and arachidonic acid (AA) by the Bron turbidimetric method. The preliminary pharmacological results showed that compounds 6b, 9b, 9d and 9h had good inhibitory effect on AA-induced platelet aggregation; compounds 6b, 6d, 6j, 9b and 9g had good inhibitory effect on ADP-induced platelet aggregation.