Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide.

Zhang HC; McComsey DF; White KB; Addo MF; Andrade-Gordon P; Derian CK; Oksenberg D; Maryanoff BE

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Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide.

机译：凝血酶受体（PAR-1）拮抗剂。通过固定在仲酰胺上，固相合成基于吲哚的肽模拟物。

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A novel, 10-step, solid-phase method, based on a secondary amide linker, was developed to construct a diverse library of indole-based SFLLR peptide mimetics as thrombin receptor (protease-activated receptor 1, PAR-1) antagonists. The key steps include stepwise reductive alkylation, urea formation, and Mannich reaction. Screening of the library led to a quick development of the SAR and the significant improvement of PAR-1 activity.

机译：开发了一种基于二级酰胺连接子的新颖的10步固相方法，以构建作为凝血酶受体（蛋白酶激活受体1，PAR-1）拮抗剂的基于吲哚的SFLLR肽模拟物的多样化文库。关键步骤包括逐步还原烷基化，尿素形成和曼尼希反应。文库的筛选导致SAR的快速发展和PAR-1活性的显着改善。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2001年第16期|共5页
作者
Zhang HC; McComsey DF; White KB; Addo MF; Andrade-Gordon P; Derian CK; Oksenberg D; Maryanoff BE;
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正文语种 eng
中图分类药学;生物化学;
关键词
Indazoles; Receptors; Thrombin; Urea; Amides; Fibrinolytic Agents; Indoles; 吲唑类; 受体; 凝血酶; 尿素;

机译：Indazoles;Receptors;Thrombin;Urea;Amides;Fibrinolytic Agents;Indoles;吲唑类;受体;凝血酶;尿素;

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1. Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide. [J] . Zhang HC, McComsey DF, White KB, Bioorganic and Medicinal Chemistry Letters . 2001,第16期

机译：凝血酶受体（PAR-1）拮抗剂。通过固定在仲酰胺上，固相合成基于吲哚的肽模拟物。
2. High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus. [J] . Zhang HC, White KB, McComsey DF, Bioorganic and Medicinal Chemistry Letters . 2003,第13期

机译：高亲和力凝血酶受体（PAR-1）配体：新一代基于吲哚的肽模拟拮抗剂，在C端带有碱性胺。
3. High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus. [J] . Zhang HC, White KB, McComsey DF, Bioorganic and Medicinal Chemistry Letters . 2003,第13期

机译：高亲和力凝血酶受体（PAR-1）配体：新一代基于吲哚的肽模拟拮抗剂，在C端带有碱性胺。
4. DESIGN AND SYNTHESIS OF A NOVEL NON-PEPTIDE MIMETIC OF PAR-1 THROMBIN RECEPTOR WITH FOUR PHARMACOPHORE GROUPS [C] . Maria Eleni Androutsou, Kostas Alexopoulos, Stefan Mihailescu the European Peptide Symposium . 2007

机译：具有四种药物组的基于PAR-1凝血酶受体的新型非肽模拟物的设计与合成
5. Design, synthesis and biological evaluation of non-hydrolyzable phosphate mimetics of receptor subtype selective LPA antagonists. [D] . McCalmont, William Forest. 2006

机译：受体亚型选择性LPA拮抗剂的不可水解磷酸盐模拟物的设计，合成和生物学评估。
6. Effects of thrombin PAR-1 activating peptide and a PAR-1 antagonist on umbilical artery resistance in vitro [O] . Aonghus J OLoughlin, Crochan J OSullivan, Nandini Ravikumar, 2005

机译：凝血酶PAR-1活化肽和PAR-1拮抗剂对体外脐动脉阻力的影响
7. Effects of thrombin, PAR-1 activating peptide and a PAR-1 antagonist on umbilical artery resistance in vitro [O] . 2005

机译：凝血酶，PAR-1活化肽和PAR-1拮抗剂对体外脐动脉阻力的影响
8. Structure-Based Design, Synthesis and Testing of Non-Peptide, Cell- Permeable, Potent Small Molecule Smac Mimetics as a New Therapy for Prostate Cancer. Revision. [R] . Wang, S. 2007

机译：基于结构的设计，合成和测试非肽，细胞渗透，有效的小分子smac模拟物作为前列腺癌的新疗法。修订。

Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide.

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