Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa.

Hanessian S; Larsson A; Fex T; Knecht W; Blomberg N

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Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa.

机译：针对凝血级联因子XIa的大环吲哚的设计与合成。

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The synthesis of a series of novel macrocyclic compounds designed to target blood coagulation Factor XIa is described. The compounds were evaluated for their inhibition of a small set of serine proteases. Several compounds displayed modest activity and good selectivity for Factor XIa. Within the series, a promising lead structure for developing novel macrocyclic inhibitors of thrombin was identified.

机译：描述了旨在靶向凝血因子XIa的一系列新型大环化合物的合成。评价化合物对一小套丝氨酸蛋白酶的抑制作用。几种化合物对因子XIa表现出适度的活性和良好的选择性。在该系列中，鉴定出了开发新型凝血酶大环抑制剂的有前途的先导结构。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第23期|共4页
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Hanessian S; Larsson A; Fex T; Knecht W; Blomberg N;
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1. Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa. [J] . Hanessian S, Larsson A, Fex T, Bioorganic and Medicinal Chemistry Letters . 2010,第23期

机译：针对凝血级联因子XIa的大环吲哚的设计与合成。
2. Design and Quantitative Structure-Activity Relationship of 3-Amidinobenzyl-1H-indole-2-carboxamides as Potent, Nonchiral, and Selective Inhibitors of Blood Coagulation Factor Xa [J] . Hans Matter, Elisabeth Defossa, Uwe Heinelt, Journal of Medicinal Chemistry . 2002,第13期

机译：3-A基苄基-1H-吲哚-2-羧酰胺作为凝血因子Xa的强，非手性和选择性抑制剂的设计及其定量构效关系
3. Design,Synthesis,and Biological Activity of Potent and Selective Inhibitors of Blood Coagulation Factor Xa [J] . J.Adam Willardsen, Danette a.Dudley, Wayne L.Cody, Journal of Medicinal Chemistry . 2004,第16期

机译：凝血因子Xa有效和选择性抑制剂的设计，合成和生物活性
4. Parameterization of Network of Blood Coagulation Cascade Including Factor Inhibiting [C] . Elena Zavyalova, Nikita Ustinov, Andrey Golovin, International Molecular Medicine Tri-Conference. . 2015

机译：血液凝固级联网络的参数化，包括因子抑制
5. The active site of membrane-bound blood coagulation factor IXa: Its location above the membrane surface and its conformational sensitivity to the factor VIIIa cofactor. [D] . Mutucumarana, Vasantha Prem. 1994

机译：膜结合凝血因子IXa的活性部位：其在膜表面上方的位置及其对因子VIIIa辅因子的构象敏感性。
6. In Silico Design of Novel Anticoagulant Peptides targeting Blood Coagulation Factor VIIa [O] . Manal S Q Al-Amri, Khalid Alrasadi, Riad Bayoumi, 2011

机译：靶向凝血因子VIIa的新型抗凝肽的计算机设计
7. Design, Synthesis and Biological Activity of Potent and Selective Inhibitors of Blood Coagulation Factor Xa [O] . -1

机译：血液凝固因子Xa效力和选择性抑制剂的设计，合成和生物活性

Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa.

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