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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
引用本文:蒋勤,孙常晟. 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[J]. 药学学报, 1990, 25(8): 598-603
作者姓名:蒋勤  孙常晟
作者单位:*江苏常州102医院;第二军医大学药学院,上海200433
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。

关 键 词:血小板聚集抑制剂  哒嗪酮
收稿时间:1989-07-06

SYNTHESIS AND PLATELET AGGREGATION INHIBITORY ACTIVITY OF 6-(4-SUBSTITUTED PHENYL)-4, 5-DIHYDRO -3(2H)-PYRIDAZINONES
Q Jiang and CS Sun. SYNTHESIS AND PLATELET AGGREGATION INHIBITORY ACTIVITY OF 6-(4-SUBSTITUTED PHENYL)-4, 5-DIHYDRO -3(2H)-PYRIDAZINONES[J]. Acta pharmaceutica Sinica, 1990, 25(8): 598-603
Authors:Q Jiang and CS Sun
Affiliation:Faculty of Pharmacy, Second Military Medical College, Shanghai.
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 piperazinyl group by cyclization of bisbromoethyl amine with 4-pyridazinonyl 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-methyl derivative of CCI-17810 (II4) was the most potent compound.
Keywords:Dihydropyridazinones  Platelet aggregation inhibitors
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