Discovery of {4-[4,9-bis(ethyloxy)-l-oxo-1,3-dihydro-2H-benzo[f] isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain

Healy Mark P.; Allan Amanda C.; Bailey Kristin; Billinton Andy; Chessell Iain P.; Clayton Nicholas M.; Giblin Gerard M. P.; Kay Melanie A.; Khaznadar Tarik; Michel Anton D.; Naylor Alan; Price Helen; Spalding David J.; Stevens David A.; Swarbrick Martin E.; Wilson Alexander W.

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Discovery of {4-[4,9-bis(ethyloxy)-l-oxo-1,3-dihydro-2H-benzo[f] isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain

【24h】

Discovery of {4-[4,9-bis(ethyloxy)-l-oxo-1,3-dihydro-2H-benzo[f] isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain

机译：发现{4- [4,9-双（乙氧基）-1-氧代-1,3-二氢-2H-苯并[F]异吲哚-2-基] -2-氟苯基}乙酸（GSK726701A），一种新颖 EP4受体部分激动剂用于治疗疼痛

获取原文

获取原文并翻译 | 示例

获取外文期刊封面目录资料

开具论文收录证明 >>

文献代查 >>

文献数据库（团队版） >>

页面导航

摘要
著录项
引文网络
相似文献
相关主题

摘要

A novel series of EP4 agonists and antagonists have been identified, and then used to validate their potential in the treatment of inflammatory pain. This paper describes these novel ligands and their activity within a number of pre-chmcal models of pain, ultimately leading to the identification of the EP4 partial agonist GSK726701A. (C) 2018 Elsevier Ltd. All rights reserved.

著录项

来源
《Bioorganic and Medicinal Chemistry Letters》 |2018年第10期|共5页
作者
Healy Mark P.; Allan Amanda C.; Bailey Kristin; Billinton Andy; Chessell Iain P.; Clayton Nicholas M.; Giblin Gerard M. P.; Kay Melanie A.; Khaznadar Tarik; Michel Anton D.; Naylor Alan; Price Helen; Spalding David J.; Stevens David A.; Swarbrick Martin E.; Wilson Alexander W.;
展开▼
作者单位

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

GlaxoSmithKline Neurosci Ctr Excellence Drug Discovery New Frontiers Sci Pk Third Ave Harlow;

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类药学;
关键词
EP4; EP4 receptor agonist; PGE2; Prostaglandin E2 receptor 4; Pam; Arthritis; Anti-inflammatory; Anti-hyperalgesic; Neuropathic pain;

机译：EP4;EP4受体激动剂;PGE2;前列腺素E2受体4;PAM;关节炎;抗炎;抗痛苦;神经性疼痛;

相似文献

外文文献
中文文献
专利

1. Discovery of {4-[4,9-bis(ethyloxy)-l-oxo-1,3-dihydro-2H-benzo[f] isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain [J] . Healy Mark P., Allan Amanda C., Bailey Kristin, Bioorganic and Medicinal Chemistry Letters . 2018,第10期

机译：发现{4- [4,9-双（乙氧基）-1-氧代-1,3-二氢-2H-苯并[F]异吲哚-2-基] -2-氟苯基}乙酸（GSK726701A），一种新颖 EP4受体部分激动剂用于治疗疼痛
2. Discovery of 4-(1-(((1-(4-(trifluoromethyl)benzyl)-1H-indol-7-yl)carbonyl)amino)cyclopropyl)be nzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain. [J] . Colucci J, Boyd M, Berthelette C, Bioorganic and Medicinal Chemistry Letters . 2010,第12期

机译：发现了高效的选择性EP4苯甲酸（4-（1-（（（1-（4-（三氟甲基）苄基）-1H-吲哚-7-基）羰基）氨基）环丙基）苯甲酸（MF-766）用于治疗炎性疼痛的拮抗剂。
3. Discovery of phenylsulfonyl acetic acid derivatives with improved efficacy and safety as potent free fatty acid receptor 1 agonists for the treatment of type 2 diabetes [J] . Zheng Li, Chunxia Liu, Xue Xu, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2017,第期

机译：发现苯磺酰乙酸衍生物具有改善的疗效和安全性，作为有效的游离脂肪酸受体1激动剂，用于治疗2型糖尿病
4. Discovery of Isoxazole Analogs of Sazetidine-A as Selective α4β2-Nicotinic Acetylcholine Receptor (nAChR) Partial Agonists for the Treatment of Depression [O] . Jianhua Liu, Li-Fang Yu, J. Brek Eaton, -1

机译：sazetidine-a的异恶唑类似物的发现作为选择性α4β2烟碱乙酰胆碱受体（naChR的）用于治疗抑郁症部分激动剂
5. GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist [O] . Wilson, Richard J, Giblin, Gerard M P, Roomans, Susan, 2009

机译：GW627368X（（N- {2- [4-（4,9-二乙氧基-1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基）苯基]乙酰基}苯磺酰胺）：新型，有效和选择性的前列腺素类EP4受体拮抗剂

Discovery of {4-[4,9-bis(ethyloxy)-l-oxo-1,3-dihydro-2H-benzo[f] isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain

摘要

著录项

引文网络

相似文献

相关主题

期刊订阅