Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation

Trotter BW; Nanda KK; Kett NR; Regan CP; Lynch JJ; Stump GL; Kiss L; Wang J; Spencer RH; Kane SA

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Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation

机译：新型异喹啉-3-腈作为口服生物可利用的Kv1.5拮抗剂的设计与合成，用于治疗房颤

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Novel 3-cyanoisoquinoline Kv1.5 antagonists have been prepared and evaluated in in vitro and in vivo assays for inhibition of the Kv1.5 potassium channel and its associated cardiac potassium current, I-Kur. Structural modifications of isoquinolinone lead 1 afforded compounds with excellent potency, selectivity, and oral bioavailability.

机译：已经制备了新颖的3-氰基异喹啉Kv1.5拮抗剂，并在体外和体内试验中评估了对Kv1.5钾通道及其相关心脏钾电流I-Kur的抑制作用。异喹啉酮铅1的结构修饰可提供具有出色效价，选择性和口服生物利用度的化合物。

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《Journal of Medicinal Chemistry》 |2006年第24期|共4页
作者
Trotter BW; Nanda KK; Kett NR; Regan CP; Lynch JJ; Stump GL; Kiss L; Wang J; Spencer RH; Kane SA;
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正文语种 eng
中图分类药学;
关键词
CARDIAC ELECTROPHYSIOLOGY; K+ CURRENT; CHANNEL; BLOCKERS; MYOCYTES; DRUGS;

机译：心脏电生理;钾离子电流;通道;阻滞剂;肌细胞;药物;

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1. Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation [J] . Trotter BW, Nanda KK, Kett NR, Journal of Medicinal Chemistry . 2006,第24期

机译：新型异喹啉-3-腈作为口服生物可利用的Kv1.5拮抗剂的设计与合成，用于治疗房颤
2. Antithrombotic therapy use in patients with atrial fibrillation before the era of non-vitamin K antagonist oral anticoagulants: the Global Registry on Long-Term Oral Antithrombotic Treatment in Patients with Atrial Fibrillation (GLORIA-AF) Phase I cohort [J] . Huisman Menno V., Ma Chang Sheng, Diener Hans-Christoph, Europace: European pacing, arrhythmias, and cardiac electrophysiology : journal of the working groups on cardiac pacing, arrhythmias, and cardiac cellular electrophysiology of the European Society of Cardiology . 2016,第9期

机译：非维生素K拮抗剂口服抗凝剂时代之前在房颤患者中使用抗血栓治疗：房颤患者长期口服抗血栓治疗的全球注册管理机构（GLORIA-AF）I期队列
3. Design and rationale of Global Registry on Long-Term Oral Antithrombotic Treatment in Patients with Atrial Fibrillation: A global registry program on long-term oral antithrombotic treatment in patients with atrial fibrillation [J] . HuismanM.V., LipG.Y.H., DienerH.C., The American heart journal . 2014,第3期

机译：心房颤动患者长期口服抗血栓治疗的全球注册管理系统的设计和原理：房颤患者长期口服抗血栓治疗的全球注册管理系统
4. What Is the Best Practical Scheme for Initiating Oral Anticoagulant Treatment in Outpatients with Atrial Fibrillation? [C] . R. CAZZIN, P. SERRA, C. FUSILLI International Workshop on Cardiac Arrhythmias . 2004

机译：在心房颤动的门诊患者中启动口服抗凝血治疗的最佳实用方案是什么？
5. Switching from Vitamin K Antagonists to Non-vitamin K Oral Anticoagulants, Drug-Drug Interactions, and Health Outcomes among Working-Age Adults with Atrial Fibrillation [D] . Feng, Xue. 2018

机译：从维生素K拮抗剂切换到非维生素K口服抗凝剂，药物 - 药物相互作用，以及具有心房颤动的工作年龄成年人之间的健康状况
6. Antithrombotic therapy use in patients with atrial fibrillation before the era of non-vitamin K antagonist oral anticoagulants: the Global Registry on Long-Term Oral Antithrombotic Treatment in Patients with Atrial Fibrillation (GLORIA-AF) Phase I cohort [O] . Menno V. Huisman, Chang Sheng Ma, Hans-Christoph Diener, -1

机译：非维生素K拮抗剂口服抗凝剂时代之前在房颤患者中使用抗血栓治疗：房颤患者长期口服抗血栓治疗全球注册表（GLORIA-AF）I队列
7. Design and Synthesis of Novel Isoquinoline-3-nitriles as Orally Bioavailable Kv1.5 Antagonists for the Treatment of Atrial Fibrillation [O] . -1

机译：新型异喹啉-3-腈的设计与合成口服生物可利用的KV1.5拮抗剂，用于治疗心房颤动

Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation

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