Considering the structural features of a group of known potent inhibitors of human platelet aggregation containing hydrazone structural backbone, a series of novel hydrazone derivatives of 2-hydrazinyl-1,3,4-thiadiazole were synthesized using a one-pot process and tested for their inhibitory activity against platelet aggregation induced by arachidonic acid and ADP. Among the derivatives, compounds 3l, 3o and 3p exhibited the highest antiplatelet aggregation activity. The derivatives were also screened for their potential antimycobacterial activity and compounds 3g, 3k, 3p and 3q were among the most active compounds.
考虑到一组已知的含有腙结构骨架的人体血小板聚集强效
抑制剂的结构特点,本研究采用一锅法合成了一系列新型 2-
肼基-1,3,4-
噻二唑腙衍
生物,并测试了它们对
花生四烯酸和
ADP 诱导的血小板聚集的抑制活性。在这些衍
生物中,化合物 3l、3o 和 3p 的抗血小板聚集活性最高。此外,还对这些衍
生物的潜在抗霉菌活性进行了筛选,结果发现 3g、3k、3p 和 3q 是活性最高的化合物。