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 molecular modeling study on their interactions with

Roma G; Di Braccio M; Grossi G; Piras D; Leoncini G; Bruzzese D; Signorello MG; Fossa P; Mosti L

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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 molecular modeling study on their interactions with

机译：新的4-（1-哌嗪基）香豆素衍生物的合成及其体外抗血小板活性。两种最有效化合物对人血小板磷酸二酯酶3的抑制特性以及与它们的相互作用的分子模型研究

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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 platelet PDE3 than milrinone and cilostazol: these data were related, through a molecular modeling study, with the molecular interactions of the four compounds with the human PDE3A catalytic site.

机译：描述了香豆素衍生物5i-x和喹啉-2（1H）-one衍生物22a，b的合成和体外抗血小板活性的重要数据，以及相应的结构活性关系。最近报道的8-甲基-4-（1-哌嗪基）-7-（3-吡啶甲氧基）香豆素5f及其有效的7-（2-吗啉代乙氧基）取代的新类似物5u比纯人血小板PDE3更有效米力农和西洛他唑：这些数据通过分子建模研究与这四种化合物与人PDE3A催化位点的分子相互作用有关。

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《Journal of Medicinal Chemistry》 |2007年第12期|共10页
作者
Roma G; Di Braccio M; Grossi G; Piras D; Leoncini G; Bruzzese D; Signorello MG; Fossa P; Mosti L;
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正文语种 eng
中图分类药学;
关键词
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE; 1; 2-FUSED PYRIMIDINES; FIELD ANALYSIS; AGGREGATION; DOCKING; AGENTS;

机译：环核苷酸磷酸酯酶;1;2-融合嘧啶;字段分析;聚集;对接;试剂;

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1. 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 molecular modeling study on their interactions with [J] . Roma G, Di Braccio M, Grossi G, Journal of Medicinal Chemistry . 2007,第12期

机译：新的4-（1-哌嗪基）香豆素衍生物的合成及其体外抗血小板活性。两种最有效化合物对人血小板磷酸二酯酶3的抑制特性以及与它们的相互作用的分子模型研究
2. Synthesis, in vitro antiplatelet activity and molecular modelling studies of 10-substituted 2-(1-piperazinyl)pyrimido[1,2-a]benzimidazol-4(10H)-ones [J] . DiBraccioM., GrossiG., SignorelloM.G., European Journal of Medicinal Chemistry: Chimie Therapeutique . 2013,第Null期

机译：10-取代的2-（1-哌嗪基）嘧啶[1,2-a]苯并咪唑-4（10H）-ones的合成，体外抗血小板活性和分子模型研究
3. Syntheses of new 3-thiazolyl coumarin derivatives, in vitro alpha-glucosidase inhibitory activity, and molecular modeling studies [J] . Salar Uzma, Taha Muhammad, Khan Khalid Mohammed, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2016,第Null期

机译：新的3-噻唑基香豆素衍生物的合成，体外α-葡萄糖苷酶抑制活性和分子模型研究
4. Docking and molecular dynamics study on the inhibitory activity of coumarins to aldose reductase [C] . Zhiguo Wang, Baoping Ling, Rui Zhang, 第四届国际分子模拟与信息技术应用学术会议（The 4th International Conference of Molecular Simulations and Applied Informatics Technologies）论文集 . 2008

机译：香豆素对醛糖还原酶抑制作用的对接和分子动力学研究
5. Interaction of excitatory and inhibitory synaptic inputs in neurons of the thalamocortical network during normal and pathological brain activity: Computational modeling and dynamic clamp in vitro [D] . Reid, Ashlan Paige 2008

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6. Synthesis and Molecular Modeling of Novel Tetrahydro-β-carboline Derivatives with Phosphodiesterase 5 Inhibitory and Anticancer Properties [O] . Heba A. Mohamed, Nancy M. R. Girgis, Rainer Wilcken, -1

机译：新型四氢β咔啉衍生物的合成和分子模拟与磷酸二酯酶5抑制和抗癌特性
7. 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 Molecular Modeling Study on Their Interactions with Phosphodiesterase 3A Catalytic Site [O] . -1

机译：新型4-（1-哌嗪基）香豆素衍生物的合成和体外抗血小板活性。人血小板磷酸二酯酶3描述的两种最有效化合物的抑制性能和分子建模研究其与磷酸二酯酶3a催化位点的相互作用
8. Studies on the Molecular Basis of Collagen-Platelet Interaction and Synthesis of Peptides that will Inhibit this Interaction [R] . Michaeli, D. 1980

机译：研究胶原 - 血小板相互作用的分子基础和抑制这种相互作用的肽的合成

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 molecular modeling study on their interactions with

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