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7-(乙氧羰基)-6,8-二甲基-2-苯基-1(2H)-酞嗪酮衍生物:合成及其对血小板聚集的抑制作用

7-(Ethoxycarbonyl)-6,8-dimethyl-2-phenyl-1(2H)-phthalazinone derivatives: synthesis and inhibitory effects on platelet aggregation.

作者信息

Sugimoto A, Tanaka H, Eguchi Y, Ito S, Takashima Y, Ishikawa M

出版信息

J Med Chem. 1984 Oct;27(10):1300-5. doi: 10.1021/jm00376a013.

Abstract

7-(Ethoxycarbonyl)-6,8-dimethyl-2-phenyl-1(2H)-phthalazinone derivatives and several analogues were synthesized and their inhibitory effects on platelet aggregation were evaluated. Structure-activity relationships are discussed. All synthesized compounds showed no appreciable effect on platelet aggregation induced by adenosine diphosphate, but most of them inhibited effectively the arachidonic acid induced platelet aggregation. The parent compound, 2-phenyl derivatives, and ortho-substituted 2-phenyl derivatives show the most potent inhibition of all compounds.

摘要

合成了7-(乙氧羰基)-6,8-二甲基-2-苯基-1(2H)-酞嗪酮衍生物及其几种类似物,并评估了它们对血小板聚集的抑制作用。讨论了构效关系。所有合成化合物对二磷酸腺苷诱导的血小板聚集均无明显作用,但其中大多数能有效抑制花生四烯酸诱导的血小板聚集。母体化合物、2-苯基衍生物和邻位取代的2-苯基衍生物在所有化合物中显示出最强的抑制作用。

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