Design and synthesis of novel platelet fibrinogen receptor antagonists with 2H-1,4-benzoxazine-3(4H)-one scaffold. A systematic study.

Anderluh M; Cesar J; Stefanic P; Kikelj D; Janes D; Murn J; Nadrah K; Tominc M; Addicks E; Giannis A; Stegnar M; Dolenc MS

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Design and synthesis of novel platelet fibrinogen receptor antagonists with 2H-1,4-benzoxazine-3(4H)-one scaffold. A systematic study.

机译：2H-1,4-苯并恶嗪-3（4H）-一个支架的新型血小板纤维蛋白原受体拮抗剂的设计与合成。有系统的研究。

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New platelet glycoprotein IIb/IIIa (GP IIb/IIIa, integrin alpha(IIb)beta3) antagonists were prepared on a 2H-1,4-benzoxazine-3(4H)-one scaffold. Their anti-aggregatory activities in human platelet rich plasma and their affinity towards alpha(IIb)beta3 and alpha(V)beta3 integrins were assessed. Various substitution positions and side chain variations were studied. In contrast to the generally accepted model, compounds containing ethyl esters as aspartate mimetics were in general more active than the corresponding free acids. We suggest an explanation for the observed behaviour of these new compounds.

机译：在2H-1,4-苯并恶嗪-3（4H）-一个支架上制备了新的血小板糖蛋白IIb / IIIa（GP IIb / IIIa，整联蛋白alpha（IIb）beta3）拮抗剂。评估了它们在富含人体血小板的血浆中的抗聚集活性以及它们对alpha（IIb）beta3和alpha（V）beta3整联蛋白的亲和力。研究了各种取代位置和侧链变化。与普遍接受的模型相反，含有乙酯作为天冬氨酸盐模拟物的化合物通常比相应的游离酸更具活性。我们建议对这些新化合物的观察行为进行解释。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2005年第1期|共25页
作者
Anderluh M; Cesar J; Stefanic P; Kikelj D; Janes D; Murn J; Nadrah K; Tominc M; Addicks E; Giannis A; Stegnar M; Dolenc MS;
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正文语种 eng
中图分类基础医学;
关键词
Blood Platelets; benzoxazine; antagonists; beta3; novel; 血小板;

机译：血小板;苯并恶嗪;拮抗剂;β3;新颖;血小板;

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1. Design and synthesis of novel platelet fibrinogen receptor antagonists with 2H-1,4-benzoxazine-3(4H)-one scaffold. A systematic study. [J] . Anderluh M, Cesar J, Stefanic P, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2005,第1期

机译：2H-1,4-苯并恶嗪-3（4H）-一个支架的新型血小板纤维蛋白原受体拮抗剂的设计与合成。有系统的研究。
2. 1,4-Benzoxazine-3(4H)-ones as Potent Inhibitors of Platelet Aggregation: Design, Synthesis and Structure–Activity Relations [J] . Chemical and Pharmaceutical Bulletin . 2014,第9期

机译：1,4-Benzoxazine-3（4H）-作为血小板聚集的强抑制剂：设计，合成和结构-活性关系
3. Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent beta(2)-adrenoceptor agonists [J] . Bioorganic and medicinal chemistry . 2020,第1期

机译：8-（2-氨基-1-羟乙基）-6-羟基-1,4-苯并恶嗪-3（4H） - 酮衍生物的设计，合成和生物学评价为有效的β（2） - 调节剂激动剂
4. Structure-activity relationship of RGD mimetics with 2H-1,4-benzoxazine-3(4H)-one scaffold [C] . Marko Anderluh, Jozko Cesar, Kristina Nadrah International Peptide Symposium;European Peptide Symposium . 2005

机译：2H-1,4-苯并恶嗪-3（4H）-NOS支架的RGD模拟物的结构 - 活性关系
5. New paradigm for drug design: Design and synthesis of novel biologically active peptides that are agonists at opioid receptors and antagonists at cholecystokinin receptors. [D] . Agnes, Richard Sario. 2003

机译：药物设计的新范例：设计和合成新型的生物活性肽，这些肽是阿片受体的激动剂，胆囊收缩素受体的拮抗剂。
6. Inhibition of platelet function with synthetic peptides designed to be high-affinity antagonists of fibrinogen binding to platelets. [O] . Z M Ruggeri, R A Houghten, S R Russell, 1986

机译：用合成肽抑制血小板功能合成肽是血纤蛋白原与血小板结合的高亲和性拮抗剂。
7. 1,4-Benzoxazine-3(4H)-ones as Potent Inhibitors of Platelet Aggregation: Design, Synthesis and Structure–Activity Relations [O] . Chang Liu, Jia-Lian Tan, Si-Yu Xiao, 2014

机译：1,4-苯并恶嗪-3（4℃） - 作为血小板聚集的有效抑制剂：设计，合成和结构 - 活动关系

Design and synthesis of novel platelet fibrinogen receptor antagonists with 2H-1,4-benzoxazine-3(4H)-one scaffold. A systematic study.

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