Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel

OlssonR.I.; JacobsonI.; IliefskiT.; Bostr?mJ.; Davidsson?.; Fjellstr?mO.; Bj?reA.; OlssonC.; SundellJ.; GranU.; GyllJ.; MalmbergJ.; Hidest?lO.; Emten?sH.; SvenssonT.; YuanZ.-Q.; StrandlundG.; ?strandA.; LindhardtE.; LinhardtG.; Forsstr?mE.; H?gberg?.; PerssonF.; AnderssonB.; R?nnborgA.; L?fbergB.

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel

【24h】

Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel

机译：内酰胺磺酰胺作为Kv1.5钾离子通道的有效抑制剂

获取原文

获取原文并翻译 | 示例

获取外文期刊封面封底 >>

开具论文收录证明 >>

文献代查 >>

团队文献服务 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

A series of lactam sulfonamides has been discovered and optimized as inhibitors of the Kv1.5 potassium ion channel for treatment of atrial fibrillation. In vitro structure-activity relationships from lead structure C to optimized structure 3y are described. Compound 3y was evaluated in a rabbit PD-model and was found to selectively prolong the atrial effective refractory period at submicromolar concentrations.

机译：已发现一系列内酰胺磺酰胺，并将其优化为Kv1.5钾离子通道抑制剂，用于治疗房颤。描述了从铅结构C到优化结构3y的体外结构活性关系。在兔PD模型中评估了化合物3y，发现该化合物在亚微摩尔浓度下选择性延长了心房有效不应期。

著录项

来源
《Bioorganic and Medicinal Chemistry Letters 》 |2014年第5期| 共5页
作者
OlssonR.I.; JacobsonI.; IliefskiT.; Bostr?mJ.; Davidsson?.; Fjellstr?mO.; Bj?reA.; OlssonC.; SundellJ.; GranU.; GyllJ.; MalmbergJ.; Hidest?lO.; Emten?sH.; SvenssonT.; YuanZ.-Q.; StrandlundG.; ?strandA.; LindhardtE.; LinhardtG.; Forsstr?mE.; H?gberg?.; PerssonF.; AnderssonB.; R?nnborgA.; L?fbergB.;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类
关键词
Atrial fibrillation; IKur; Kv1.5; Lactams; Sulfonamides;

机译：心房颤动;IKur;Kv1.5;内酰胺;磺酰胺;

相似文献

外文文献
中文文献
专利

1. Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel [J] . OlssonR.I., JacobsonI., IliefskiT., Bioorganic and Medicinal Chemistry Letters . 2014 ,第5期

机译：内酰胺磺酰胺作为Kv1.5钾离子通道的有效抑制剂
2. Comparison of potent Kv1.5 potassium channel inhibitors reveals the molecular basis for blocking kinetics and binding mode [J] . Strutz-Seebohm N, Gutcher I, Decher N, Cellular Physiology and Biochemistry . 2007 ,第6期

机译：比较有效的Kv1.5钾通道抑制剂可揭示阻断动力学和结合方式的分子基础
3. Inhibition of 15-lipoxygenase (15-LOX) reverses hypoxia-induced down-regulation of potassium channels Kv1.5 and Kv2.1Inhibition of 15-lipoxygenase (15-LOX) reverses hypoxia-induced down-regulation of potassium channels Kv1.5 and Kv2.1 [J] . Wenjuan Liu, Di Wang, Kaibin Song, International Journal of Clinical and Experimental Medicine . 2014 ,第11期

机译：抑制15-脂氧合酶（15-LOX）逆转缺氧诱导的钾通道Kv1.5和Kv2.1的抑制抑制15-脂氧合酶（15-LOX）逆转低氧诱导下调的钾离子通道Kv1.5和Kv2.1 Kv2.1
4. A Multiplatform Strategy for the Discovery of Conventional Monoclonal Antibodies That Inhibit the Voltage-Gated Potassium Channel Kvl.3. [C] . Yelena Bisharyan, J. Bednenko, R. Harriman, Protein Engineering Summit. . 2018

机译：一种抑制电压门控钾通道KVL的常规单克隆抗体的多平台策略。
5. Progress toward the total synthesis of correolide: A potent and selective Kv1.3 potassium ion channel inhibitor. [D] . Roth, Joshua John. 2006

机译：全合成Correolide的进展：一种有效的选择性Kv1.3钾离子通道抑制剂。
6. Inhibition of 15-lipoxygenase (15-LOX) reverses hypoxia-induced down-regulation of potassium channels Kv1.5 and Kv2.1Inhibition of 15-lipoxygenase (15-LOX) reverses hypoxia-induced down-regulation of potassium channels Kv1.5 and Kv2.1 [O] . Wenjuan Liu, Di Wang, Kaibin Song, 2014

机译：抑制15-脂氧合酶（15-LOX）逆转低氧诱导的钾通道Kv1.5和Kv2.1的抑制抑制15-脂氧合酶（15-LOX）逆转低氧诱导的钾通道Kv1.5和Kv2.1的向下调节。 Kv2.1
7. Comparison of potent Kv1.5 potassium channel inhibitors reveals the molecular basis for blocking kinetics and binding mode [O] . Strutz-Seebohm, Nathalie, Gutcher, Ilona, Decher, Niels, 2007

机译：比较有效的Kv1.5钾通道抑制剂可揭示阻断动力学和结合方式的分子基础

Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel

摘要

著录项

相似文献

相关主题

期刊订阅