Synthesis and In Vitro Antiplatelet Activity of New 4-(1-Piperazinyl)coumarin Derivatives. Human Platelet Phosphodiesterase 3 Inhibitory Properties of the Two Most Effective Compounds Described and Mo

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• 作者：Giorgio Roma ; Mario Di Braccio ; Giancarlo Grossi ; Daniela Piras ; Giuliana Leoncini ; Debora Bruzzese ; Maria Grazia Signorello ; Paola Fossa ; Luisa Mosti
• 刊名：Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：June 14, 2007
• 年：2007
• 卷：50
• 期：12
• 页码：2886 - 2895
• 全文大小：494K
• 年卷期：v.50,no.12(June 14, 2007)
• ISSN：1520-4804

文摘

The synthesis and in vitro antiplatelet activity significant data of coumarin derivatives 5i-x and quinolin-2(1H)-one derivatives 22a,b, as well as the corresponding structure-activity relationships are described.The recently reported 8-methyl-4-(1-piperazinyl)-7-(3-pyridylmethoxy)coumarin 5f and its potent 7-(2-morpholinoethoxy)-substituted new analogue 5u were notably more effective inhibitors of pure human plateletPDE3 than milrinone and cilostazol: these data were related, through a molecular modeling study, with themolecular interactions of the four compounds with the human PDE3A catalytic site.