6-取代二氢哒嗪酮的合成及其血小板聚集抑制活性

[Synthesis and platelet aggregation inhibitory activity of 6-substituted dihydropyridazinones].

作者信息

Yao F M, Sun C S

机构信息

Department of Pharmacy, Bethune International Peace Hospital, Shijiazhuang.

出版信息

Yao Xue Xue Bao. 1993;28(7):548-52.

Abstract

In order to develop more potent and less toxic antithrombotic agents, ten 6-(4-substituted piperazinyl acetyl aminophenyl)-4,5-dihydro-3(2H)-pyridazinones were synthesized. The title compounds were tested in vitro for platelet aggregation inhibitory activity with ADP-induced rat platelets and PAF-induced rabbit platelets. Preliminary tests showed that all of the pyridazinones could inhibit ADP-induced rat platelet aggregation. I7, I8, I9 were more potent than the control compound CI 930. I9 was the most potent compound with IC50 of 0.99 mumol/L. Pertaining to PAF-induced rabbit platelet aggregation, I9 was the most potent inhibitor with IC50 of 3.7 mumol/L.

摘要

为了开发出更有效且毒性更低的抗血栓形成药物，合成了10种6-(4-取代哌嗪基乙酰氨基苯基)-4,5-二氢-3(2H)-哒嗪酮。用ADP诱导的大鼠血小板和PAF诱导的兔血小板对标题化合物进行了体外血小板聚集抑制活性测试。初步测试表明，所有哒嗪酮均可抑制ADP诱导的大鼠血小板聚集。I7、I8、I9比对照化合物CI 930更有效。I9是最有效的化合物，IC50为0.99 μmol/L。对于PAF诱导的兔血小板聚集，I9是最有效的抑制剂，IC50为3.7 μmol/L。

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