The identification of orally bioavailable thrombopoietin agonists.

Munchhof MJ; Antipas AS; Blumberg LC; Brissette WH; Brown MF; Casavant JM; Doty JL; Driscoll J; Harris TM; Wolf Gouveia LA; Jones CS; Li Q; Linde RG; Lira PD; Marfat A; McElroy E; Mitton Fry M; McCurdy SP; Reiter LA; Ripp SL; Shavnya A; Thomasco LM; Trevena KA

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The identification of orally bioavailable thrombopoietin agonists.

机译：口服生物利用性血小板生成素激动剂的鉴定。

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Recently, we disclosed a series of potent pyrimidine benzamide-based thrombopoietin receptor agonists. Unfortunately, the structural features required for the desired activity conferred physicochemical properties that were not favorable for the development of an oral agent. The physical properties of the series were improved by replacing the aminopyrimidinyl group with a piperidine-4-carboxylic acid moiety. The resulting compounds possessed favorable in vivo pharmacokinetic properties, including good bioavailability.

机译：最近，我们公开了一系列有效的基于嘧啶苯甲酰胺的血小板生成素受体激动剂。不幸的是，所需活性所需的结构特征赋予了不利于口服剂开发的物理化学性质。通过用哌啶-4-羧酸部分取代氨基嘧啶基改善了该系列的物理性质。所得化合物具有良好的体内药代动力学特性，包括良好的生物利用度。

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《Bioorganic and Medicinal Chemistry Letters》 |2009年第5期|共3页
作者
Munchhof MJ; Antipas AS; Blumberg LC; Brissette WH; Brown MF; Casavant JM; Doty JL; Driscoll J; Harris TM; Wolf Gouveia LA; Jones CS; Li Q; Linde RG; Lira PD; Marfat A; McElroy E; Mitton Fry M; McCurdy SP; Reiter LA; Ripp SL; Shavnya A; Thomasco LM; Trevena KA;
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1. The identification of orally bioavailable thrombopoietin agonists. [J] . Munchhof MJ, Antipas AS, Blumberg LC, Bioorganic and Medicinal Chemistry Letters . 2009,第5期

机译：口服生物利用性血小板生成素激动剂的鉴定。
2. Discovery of potent, selective, and orally bioavailable 3H-spiro(isobenzofuran-1,4'-piperidine) based melanocortin subtype-4 receptor agonists. [J] . Guo L, Ye Z, Liu J, Bioorganic and Medicinal Chemistry Letters . 2010,第16期

机译：发现有效，选择性和口服生物可利用的3H-螺螺（Isobenzofuran-1,4'-哌啶）的基于Melanocortin亚型-4受体激动剂。
3. Discovery of potent, selective, and orally bioavailable 3H-spiro(isobenzofuran-1,4'-piperidine) based melanocortin subtype-4 receptor agonists. [J] . Guo L, Ye Z, Liu J, Bioorganic and Medicinal Chemistry Letters . 2010,第16期

机译：发现有效，选择性和口服生物利用的3H-螺（异苯并呋喃-1,4'-哌啶）的黑皮质素亚型4受体激动剂。
4. Asenic oral bioavailability in soils,housedust,and food:implications forr human health [C] . L.Q.Ma, H.B.Li, D.Zhao International Congress and Exhibition on Arsenic in the Environment . 2019

机译：土壤，房屋粉尘和食物中的砷口腔生物利用度：对人类健康的影响
5. Physical Characterization, Metal-binding Kinetics and in Vivo Efficacy of an Orally Bioavailable Chelating Agent [D] . Coste Sanchez, Carla. 2019

机译：物理特征，金属结合动力学和口服生物可利用螯合剂的体内疗效
6. Identification of the Residues in the Extracellular Domain of Thrombopoietin Receptor Involved in the Binding of Thrombopoietin and a Nuclear Distribution Protein (Human NUDC) [O] . Wei-Min Chen, Bo Yu, Qing Zhang, 2010

机译：血小板生成素受体的胞外域中涉及血小板生成素与核分布蛋白（人类NUDC）结合的残基的鉴定
7. Discovery of the a7 Nicotinic Acetylcholine Receptor Agonists. (R)-3-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo2.2.2octane-3, 5-1, 3oxazolidin-2-one as a Novel, Potent, Selective, and Orally Bioavailable Ligand [O] . -1

机译：发现A7烟碱乙酰胆碱受体激动剂。（r）-3-（5-氯噻吩-2-基）螺旋-1- azabocyclo 2.2.2辛烷-3，5- 1,3恶唑烷-2-单，为新型，有效，选择性和口服生物可利用的配体
8. Bioavailability of Oral Pyridostigmine and Inhibition of Red Blood Cell Acetylcholinesterase by Oral and Intravenous Pyridostigmine. Final Report October 21, 1985-March 22, 1989 [R] . Kornhouser, D. M., Petty, B. G., Lietman, P. S. 1989

机译：口服吡啶斯的明生物利用度和口服和静脉注射吡啶斯的明对红细胞乙酰胆碱酯酶的抑制作用。最终报告1985年10月21日至1989年3月22日

The identification of orally bioavailable thrombopoietin agonists.

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