Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A<sub>2</sub> Type X (sPLA<sub>2</sub>-X) Inhibitors

Laurent Knerr; Fabrizio Giordanetto; Peter Nordberg; Daniel Pettersen; Nidhal Selmi; Hans-Georg Beisel; Hannah de la Motte; Thomas Olsson; Tim D. J. Perkins; Margareta Hersl?f; ?sa M?nsson; Mikael Dahlstr?m; Ingemar Starke; Johan Broddefalk; Gabrielle Saarinen; Fredrik Klingeg?rd; Eva Hurt-Camejo; Birgitta Rosengren; Johan Brengdahl; Frank Jansen; Mattias Rohman; Jenny Sandmark; Kenth Hallberg; Tomas ?kerud; Robert G. Roth; Marie Ahlqvist

首页> 外文期刊>ACS medicinal chemistry letters >Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A₂ Type X (sPLA₂-X) Inhibitors

【24h】

Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A₂ Type X (sPLA₂-X) Inhibitors

机译：发现一系列吲哚-2甲酰胺作为选择性分泌的磷脂酶A _{2 型X（SPLA _{2 -X）抑制剂}}

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

In order to assess the potential of sPLA_(2)-X as a therapeutic target for atherosclerosis, novel sPLA_(2) inhibitors with improved type X selectivity are required. To achieve the objective of identifying such compounds, we embarked on a lead generation effort that resulted in the identification of a novel series of indole-2-carboxamides as selective sPLA2-X inhibitors with excellent potential for further optimization.

机译：为了评估SPLA_（2）-X作为动脉粥样硬化的治疗靶的潜力，需要具有改进的X选择性的新型SPLA_（2）抑制剂。为了达到鉴定这些化合物的目的，我们开始了潜在的良好努力，导致鉴定新型吲哚-2-甲酰胺系列作为选择性SPLA2-X抑制剂，具有出于进一步优化的优异潜力。

著录项

来源
《ACS medicinal chemistry letters》 |2018年第7期|共6页
作者
Laurent Knerr; Fabrizio Giordanetto; Peter Nordberg; Daniel Pettersen; Nidhal Selmi; Hans-Georg Beisel; Hannah de la Motte; Thomas Olsson; Tim D. J. Perkins; Margareta Hersl?f; ?sa M?nsson; Mikael Dahlstr?m; Ingemar Starke; Johan Broddefalk; Gabrielle Saarinen; Fredrik Klingeg?rd; Eva Hurt-Camejo; Birgitta Rosengren; Johan Brengdahl; Frank Jansen; Mattias Rohman; Jenny Sandmark; Kenth Hallberg; Tomas ?kerud; Robert G. Roth; Marie Ahlqvist;
展开▼
作者单位

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

Reagents and Assay Development Mechanistic Biology and Profiling and Structure and Biophysics;

Reagents and Assay Development Mechanistic Biology and Profiling and Structure and Biophysics;

Reagents and Assay Development Mechanistic Biology and Profiling and Structure and Biophysics;

Reagents and Assay Development Mechanistic Biology and Profiling and Structure and Biophysics;

Reagents and Assay Development Mechanistic Biology and Profiling and Structure and Biophysics;

Reagents and Assay Development Mechanistic Biology and Profiling and Structure and Biophysics;

Reagents and Assay Development Mechanistic Biology and Profiling and Structure and Biophysics;

Medicinal Chemistry Translational Sciences Bioscience and Drug Metabolism and Pharmacokinetics;

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类药学;化学;
关键词
atherosclerosis; coronary artery disease; inhibitor; Secreted phospholipase A2 type X; X-ray crystallography;

机译：动脉粥样硬化;冠状动脉疾病;抑制剂;分泌的磷脂酶A2型X;X射线晶体学;
入库时间 2022-08-20 00:55:27

相似文献

外文文献
中文文献
专利

1. Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A₂ Type X (sPLA₂-X) Inhibitors [J] . Laurent Knerr, Fabrizio Giordanetto, Peter Nordberg, ACS medicinal chemistry letters . 2018,第7期

机译：发现一系列吲哚-2甲酰胺作为选择性分泌的磷脂酶A _{2 型X（SPLA _{2 -X）抑制剂}}
2. Blockade of Human Group X Secreted Phospholipase A2 (GX-sPLA2)-induced Airway Inflammation and Hyperresponsiveness in a Mouse Asthma Model by a Selective GX-sPLA2 Inhibitor [J] . William R. Henderson, Rob Oslund, James Bollinger, The Journal of biological chemistry . 2011,第32期

机译：通过选择性GX-SPRA2抑制剂阻断人组X分泌的磷脂酶A2（GX-SPLA2）诱导的气道炎症和小鼠哮喘模型的高反应性
3. Discovery of AZD2716: A Novel Secreted Phospholipase A(2) (sPLA(2)) Inhibitor for the Treatment of Coronary Artery Disease [J] . Giordanetto Fabrizio, Pettersen Daniel, Starke Ingemar, ACS medicinal chemistry letters . 2016,第10期

机译：AZD2716的发现：一种新型的分泌型磷脂酶A（2）（sPLA（2））抑制剂用于治疗冠状动脉疾病
4. Potent and selective 2-oxoamide inhibitors of phospholipases A2 as novel medicinal agents for the treatment of inflammatory diseases [C] . Efrosini Barbayianni, Georgia Antonopoulou, George Kokotos IUPAC World Congress on Chemistry . 2015

机译：磷脂酶A2的有效和选择性的2-氧代咪唑抑制剂作为治疗炎性疾病的新型药剂
5. Application of organocatalysis to the synthesis of chiral morpholines, piperazines, aziridines, azetidines, beta-fluoroamines, and gamma-fluoroamines; discovery of selective phospholipase D inhibitors with optimized in vivo properties. [D] . O'Reilly, Matthew C. 2014

机译：有机催化在合成手性吗啉，哌嗪，氮丙啶，氮杂环丁烷，β-氟胺和γ-氟胺中的应用；发现具有优化体内特性的选择性磷脂酶D抑制剂。
6. Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors [O] . Laurent Knerr, *, Fabrizio Giordanetto, 2018

机译：发现一系列作为选择性分泌磷脂酶A2型X（sPLA2-X）抑制剂的吲哚2羧酰胺。
7. Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors [O] . Laurent Knerr, Fabrizio Giordanetto, Peter Nordberg, 2018

机译：发现一系列吲哚-2甲酰胺作为选择性分泌的磷脂酶A2型X（SPLA2-X）抑制剂

Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors

摘要

著录项

相似文献

相关主题

期刊订阅

Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A₂ Type X (sPLA₂-X) Inhibitors