Discovery of an Orally Efficacious Inhibitor of Coagulation Factor Xa Which Incorporates a Neutral P_1 Ligand

Yong Mi Choi-Sledeski; Robert Kearney; Gregory Poli; Henry Pauls; Charles Gardner; Yong Gong; Michael Becker; Roderick Davis; Alfred Spada; Guyan Liang

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Discovery of an Orally Efficacious Inhibitor of Coagulation Factor Xa Which Incorporates a Neutral P_1 Ligand

机译：发现具有中性P_1配体的凝血因子Xa口服有效抑制剂。

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The discovery and SAR of ketopiperazino methylazaindole factor Xa inhibitors are described. Structure-activity data suggesting that this class of inhibitors does not bind in the canonical mode were confirmed by an X-ray crystal structure showing the neutral haloaromatic bound in the S_1 subsite. The most potent azaindole, 33 (RPR209685), is selective against related serine proteases and attains higher levels of exposure upon oral dosing than comparable benzamidines and benzamidine isosteres. Compound 33 was efficacious in the canine AV model of thrombosis.

机译：描述了酮哌嗪子基甲基氮杂吲哚因子Xa抑制剂的发现和SAR。结构活性数据表明这种抑制剂不以规范模式结合，这是通过X射线晶体结构证实的，该结构显示在S_1亚位点中性卤代芳香族结合。最有效的氮杂吲哚（33）（RPR209685）对相关的丝氨酸蛋白酶具有选择性，并且在口服给药时与可比的苯甲am和苯甲oster等排物相比具有更高的暴露水平。化合物33在犬AV模型血栓形成中有效。

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《Journal of Medicinal Chemistry》 |2003年第5期|共4页
作者
Yong Mi Choi-Sledeski; Robert Kearney; Gregory Poli; Henry Pauls; Charles Gardner; Yong Gong; Michael Becker; Roderick Davis; Alfred Spada; Guyan Liang;
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1. Discovery of an Orally Efficacious Inhibitor of Coagulation Factor Xa Which Incorporates a Neutral P_1 Ligand [J] . Yong Mi Choi-Sledeski, Robert Kearney, Gregory Poli, Journal of Medicinal Chemistry . 2003,第5期

机译：发现具有中性P_1配体的凝血因子Xa口服有效抑制剂。
2. The syntheses and in vitro biotransformation studies of (~14C)apixaban, a highly potent, selective, efficacious and orally bioawailable inhibitor of blood coagulation Factor Xa [J] . Brad D. Maxwell, Scott B. Tran, Shiang Yuan Chen, Journal of Labelled Compounds and Radiopharmaceuticals . 2011,第7a8期

机译：（〜14C）apixaban的合成及体外生物转化研究，一种高效，选择性，有效且可口服的生物可凝血因子Xa抑制剂
3. The syntheses and in vitro biotransformation studies of (~14C)apixaban, a highly potent, selective, efficacious and orally bioawailable inhibitor of blood coagulation Factor Xa [J] . Brad D. Maxwell, Scott B. Tran, Shiang Yuan Chen, Journal of Labelled Compounds and Radiopharmaceuticals . 2011,第7a8期

机译：（〜14C）甲苯的合成和体外生物转化研究，一种高效，选择性，有效和口服的血液凝固因子Xa的生物可抑制剂
4. Assessment of the efficacy of tissue factor pathway inhibitor (TFPI) immobilized on glass slides to inhibit factor Xa under flow conditions [C] . Chandiwal, A., Mast, . 2002

机译：评估流动条件下固定在载玻片上的组织因子途径抑制剂（TFPI）抑制Xa因子的功效
5. Inhibitor discovery against blood coagulation factor Xa and Bacillus anthracis protective antigen. [D] . Lee, Oukseub. 2009

机译：针对凝血因子Xa和炭疽芽孢杆菌保护性抗原的抑制剂发现。
6. Discovery of aChemical Probe Bisamide (CCT251236):An Orally Bioavailable Efficacious Pirin Ligand from a Heat ShockTranscription Factor 1 (HSF1) Phenotypic Screen [O] . MatthewD. Cheeseman, Nicola E. A. Chessum, Carl S. Rye, -1

机译：发现一个化学探针双酰胺（CCT251236）：热休克口服生物有效的Pirin配体转录因子1（HSF1）表型筛选
7. Effects of the oral, direct factor Xa inhibitor apixaban on routine coagulation assays and anti-Xa assays. [O] . Hillarp, Andreas, Gustafsson, Kerstin M, Faxälv, Lars, 2014

机译：口服，直接因子Xa抑制剂阿哌沙班对常规凝血试验和抗Xa试验的影响。

Discovery of an Orally Efficacious Inhibitor of Coagulation Factor Xa Which Incorporates a Neutral P_1 Ligand

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