论文部分内容阅读
以吡考他胺为先导化合物,依据生物电子等排体原理,设计并合成了3个标题化合物,所有化合物均未见文献报道,其结构均经IR、1HNMR、13CNMR和MS确证。采用Bron比浊法测定了标题化合物对腺苷二磷酸(Adenosine diphosphate,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,标题化合物对ADP诱导的血小板聚集均具有显著的抑制活性,其中4-甲氧基-N1,N3-二((3,5,6-三甲基吡嗪-2-基)甲基)间苯二甲酰胺和4-甲氧基-N1,N3-二((5-甲基吡嗪)-2-亚甲基)间苯二甲酰胺对AA诱导的血小板聚集也显示出较强的抑制活性。
Pichotamine was taken as the lead compound. Based on the principle of bioisostere, three title compounds were designed and synthesized. All the compounds were not reported in the literature. Their structures were confirmed by IR, 1HNMR, 13CNMR and MS. The inhibitory activity of the title compound against platelet aggregation induced by adenosine diphosphate (ADP) and arachidonic acid (AA) was determined by the bronchial turbidimetry. The preliminary pharmacological results show that the title compound has significant inhibitory activity on ADP-induced platelet aggregation, in which 4-methoxy-N1, N3-bis ((3,5,6-trimethylpyrazin- Methyl) isophthalamide and 4-methoxy-N1, N3-bis ((5-methylpyrazine) -2-methylene) isophthalamide also showed AA-induced platelet aggregation Strong inhibitory activity.