1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.

Jia ZJ; Wu Y; Huang W; Zhang P; Song Y; Woolfrey J; Sinha U; Arfsten AE; Edwards ST; Hutchaleelaha A; Hollennbach SJ; Lambing JL; Scarborough RM; Zhu BY

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.

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1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.

机译：1-（2-萘基）-1H-吡唑-5-羧酰胺作为有效的Xa因子抑制剂。第3部分：口服生物可用的苯甲idine-P4抑制剂的设计，合成和SAR。

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Using N,N-dialkylated benzamidines as the novel P4 motifs, we have designed and synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent and selective fXa inhibitors with significantly improved hydrophilicity and in vitro anticoagulant activity. These benzamidine-P4 fXa inhibitors have displayed excellent oral bioavailability and long half-life.

机译：使用N，N-二烷基化的苯甲idine作为新颖的P4基序，我们设计并合成了一类1-（2-萘基）-1H-吡唑-5-羧酰胺类化合物，它们是高效，选择性的fXa抑制剂，具有明显改善的亲水性和体外作用抗凝活性。这些苯甲idine-P4 fXa抑制剂具有出色的口服生物利用度和长半衰期。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2004年第5期|共6页
作者
Jia ZJ; Wu Y; Huang W; Zhang P; Song Y; Woolfrey J; Sinha U; Arfsten AE; Edwards ST; Hutchaleelaha A; Hollennbach SJ; Lambing JL; Scarborough RM; Zhu BY;
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正文语种 eng
中图分类基础医学;
关键词
inhibitors; pyrazole; benzamidine; bioavailable; Part;

机译：抑制剂;吡唑;苯甲m;生物利用度;部分;

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1. 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors. [J] . Jia ZJ, Wu Y, Huang W, Bioorganic and Medicinal Chemistry Letters . 2004,第5期

机译：1-（2-萘基）-1H-吡唑-5-羧酰胺作为有效的Xa因子抑制剂。第3部分：口服生物可用的苯甲idine-P4抑制剂的设计，合成和SAR。
2. Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides. [J] . Jia ZJ, Wu Y, Huang W, Bioorganic and Medicinal Chemistry Letters . 2002,第12期

机译：新型非-因子Xa抑制剂的设计，合成和生物学活性。第1部分：取代的1-（2-萘基）-1H-吡唑-5-羧酰胺的P（1）结构-活性关系。
3. Design, synthesis, and SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part I: exploration of 5-6 fused rings as alternative S1 moieties. [J] . Yoshikawa K, Yokomizo A, Naito Bioorganic and medicinal chemistry . 2009,第24期

机译：设计，合成和合成作为有效Xa抑制剂的顺式1,2-二氨基环己烷衍生物。第一部分：探索5-6个稠环作为S1的替代部分。
4. Part I. Synthetic efforts towards a total synthesis of Haterumalide NA/Oocydin A. Part II. Deciphering the coupling constants of Spiruchostatins A and B. Part III. Design and synthesis of analogs of Latrunculin A and B, potent actin polymerization inhibitors. [D] . Wang, Jizhou. 2005

机译：第一部分：为完全合成Haterumalide NA / Oocydin A的合成努力。第二部分。破译螺旋藻抑素A和B的偶联常数。第三部分。设计和合成Latrunculin A和B，强肌动蛋白聚合抑制剂的类似物。
5. Design Synthesis and SAR Studies of 4-Substituted Methoxylbenzoyl-aryl-thiazoles Analogues as Potent and Orally Bioavailable Anticancer Agents [O] . Yan Lu, Chien-Ming Li, Zhao Wang, -1

机译：4-取代methoxylbenzoyl芳基噻唑类似物作为强有力的和口服生物抗癌药物设计合成和saR研究
6. Design, Synthesis and Discovery of 1-(2-(6-Chloro-3-methylsulfonyl)-naphthyl)-1H-pyrazole-5-carboxylamides as Highly Potent Factor Xa Inhibitors [O] . Zhaozhong Jon Jia, Robert Murry Scarborough, Penglie Zhang, 2009

机译：设计，合成和发现1-（2-（6-氯-3-甲基磺酰基） - 萘基）-1H-吡唑-5-羧基，如高效因子XA抑制剂

1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.

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