6-(4-取代苯基)-4,5-二氢-3(2H)-哒嗪酮类化合物的合成及其抑制血小板聚集的作用

SYNTHESIS AND PLATELET AGGREGATION INHIBITORY ACTIVITY OF 6-(4-SUBSTITUTED PHENYL)-4, 5-DIHYDRO -3(2H)-PYRIDAZINONES

摘要: 为了寻找较理想的抗血栓药物,本文设计合成了6-(4-取代苯基)-4,5-二氢-3(2H)-哒嗪酮类化合物16个。对ADP诱导的大鼠体外血小板聚集,均有不同程度的抑制作用。其中,化合物Ⅱ₂,Ⅱ3和Ⅱ₄的作用大于CCI-17810,又以Ⅱ₄的作用为最强。

Abstract: To search for more ideal antithrombotic drugs sixteen 6-(4-substituted phenyl)-4, 5-dihydro-3(2H)-pyridazinones were designed and synthesized. Some. improvement of the synthetic method involved in constructing the piperazinyi group by cyclization of bisbromoethyl amine with 4-pyridazin0nyl anilines.Preliminary pharmacological tests showed that all of the target compounds inhibited ADP induced platelet aggregation. Compounds Ⅱ₂, Ⅱ₃ and Ⅱ₄ were more potent than CCI-17810. The 5-methylderivative of CCI-17810 (Ⅱ₄) was the most potent compound.