首页> 美国卫生研究院文献>other >Discovery synthesis and SAR analysis of novel selective small molecule S1P4–R agonists based on a (2Z5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype

【2h】

Discovery synthesis and SAR analysis of novel selective small molecule S1P4–R agonists based on a (2Z5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype

机译：基于（2Z5Z）-5 - （（Pyrol-3-基）亚甲基）-3-烷基-2-（烷基-2-（烷基氨基）噻唑烷-4- 4 - 基于（2Z5Z）-5 - （（吡咯-3-基）-2-（烷基-2-（烷基氨基）的新选择性小分子S1P4-R激动剂的发现合成和SAR分析。一个趋化型

代理获取

本网站仅为用户提供外文OA文献查询和代理获取服务，本网站没有原文。下单后我们将采用程序或人工为您竭诚获取高质量的原文，但由于OA文献来源多样且变更频繁，仍可能出现获取不到、文献不完整或与标题不符等情况，如果获取不到我们将提供退款服务。请知悉。

页面导航

摘要
著录项
相似文献
相关主题

摘要

High affinity and selective S1P4 receptor (S1P4–R) small molecule agonists may be important proof-of-principle tools used to clarify the receptor biological function and effects to assess the therapeutic potential of the S1P4–R in diverse disease areas including treatment of viral infections and thrombocytopenia. A high-throughput screening campaign of the Molecular Libraries-Small Molecule Repository was carried out by our laboratories and identified (2Z,5Z)-5-((1-(2-fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)methylene)-3-methyl-2-(methylimino) thiazolidin-4-one as a promising S1P4–R agonist hit distinct from literature S1P4–R modulators. Rational chemical modifications of the hit allowed the identification of a promising lead molecule with low nanomolar S1P4–R agonist activity and exquisite selectivity over the other S1P1-3,5–Rs family members. The lead molecule herein disclosed constitutes a valuable pharmacological tool to explore the effects of the S1P4–R signaling cascade and elucidate the molecular basis of the receptor function.

著录项

期刊名称 other
作者
Mariangela Urbano; Miguel Guerrero; Subash Velaparthi; Melissa Crisp; Peter Chase; Peter Hodder; Marie-Therese Schaeffer; Steven Brown; Hugh Rosen; Edward Roberts;
展开▼
作者单位

展开▼
年(卷),期 -1(21),22
年度 -1
页码 6739–6745
总页数 20
原文格式 PDF
正文语种
中图分类
关键词
S1P4 receptor selective small molecule S1P4–R agonists thrombocytopenia viral infections;

机译：S1P4受体;选择性小分子S1P4-R激动剂;血小板减少症;病毒感染;

相似文献

外文文献
中文文献
专利

1. Discovery, synthesis and SAR analysis of novel selective small molecule S1P 4-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3- alkyl-2-(alkylimino)thiazolidin-4-one chemotype [J] . UrbanoM., GuerreroM., VelaparthiS., Bioorganic and Medicinal Chemistry Letters . 2011,第22期

机译：基于（2Z，5Z）-5-（（吡咯-3-基）亚甲基）-3-烷基-2-（烷基亚氨基）噻唑烷-4的新型选择性小分子S1P 4-R激动剂的发现，合成和SAR分析一化学型
2. Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties. [J] . Marx IE, DiMauro EF, Cheng A, Bioorganic and Medicinal Chemistry Letters . 2009,第1期

机译：发现作为CB2的强效和选择性激动剂的α-酰胺基砜：合成，SAR和药代动力学特性。
3. Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan. [J] . Kamei K, Maeda N, Nomura K, Bioorganic and Medicinal Chemistry . 2006,第6期

机译：具有神经保护作用的选择性5-HT1A受体激动剂1,4-苯并氮杂ze庚因衍生物的合成，SAR研究和评估：Piclozotan的发现。
4. SAR Analysis of Innovative Selective Small Molecule Antagonists of Sphingosine-1-Phosphate 4 (S1P4) Receptor [O] . Mariangela Urbano, Miguel Guerrero, Jian Zhao, -1

机译：SAR分析鞘氨酸-1-磷酸三种磷酸三种（S1P4）受体的创新选择性小分子拮抗剂
5. Discovery, synthesis and SAR analysis of novel selective small molecule S1P4-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype [O] . Mariangela Urbano, Miguel Guerrero, Subash Velaparthi, 2011

机译：基于（2Z，5Z）-5 - （（Pyrol-3-基）亚甲基）-3-烷基-2-（烷基-2-（烷基氨基）噻唑烷-4- 4 - 基于（2Z，5Z）-5 - （（吡咯-3-基）-2-（烷基-2-（烷基氨基）的新选择性小分子S1P4-R激动剂的发现，合成和SAR分析。一个趋化型

Discovery synthesis and SAR analysis of novel selective small molecule S1P4–R agonists based on a (2Z5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype

摘要

著录项

相似文献

相关主题

期刊订阅