Synthesis and inhibitory activity on hepatitis C virus RNA replication of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxy-2-propyl)aniline analogs

MatsunoK.; UedaY.; FukudaM.; OnodaK.; WakiM.; IkedaM.; KatoN.; MiyachiH.

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Synthesis and inhibitory activity on hepatitis C virus RNA replication of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxy-2-propyl)aniline analogs

机译：4-（1,1,1,3,3,3-六氟-2-羟基-2-丙基）苯胺类似物的丙型肝炎病毒RNA复制的合成及其抑制活性

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Using our recently developed assay system for full-genome-length hepatitis C virus (HCV) RNA replication in human hepatoma-derived Li23 cells (ORL8), we identified 4-(1,1,1,3,3,3-hexafluoro-2-hydroxy-2-propyl)aniline analog 1a as a novel HCV inhibitor. Structural modifications of 1a provided a series of sulfonamides 7 with much more potent HCV RNA replication-inhibitory activity than ribavirin. Compound 7a showed an additive anti-HCV effect in combination with standard anti-HCV therapy (IFN-α plus ribavirin). Since 7a generated reactive oxygen species (ROS) in the ORL8 system and its anti-HCV activity was blocked by vitamin E, its anti-HCV activity may be mediated at least in part by ROS.

机译：使用我们最近开发的用于全基因组丙型肝炎病毒（HCV）RNA在人肝癌衍生的Li23细胞（ORL8）中复制的测定系统，我们确定了4-（1,1,1,3,3,3-hexafluoro- 2-羟基-2-丙基）苯胺类似物1a作为新型HCV抑制剂。 1a的结构修饰为一系列磺酰胺7提供了比利巴韦林更有效的HCV RNA复制抑制活性。化合物7a与标准抗HCV治疗（IFN-α加利巴韦林）组合显示出加性抗HCV作用。由于7a在ORL8系统中生成了活性氧（ROS），并且其抗HCV活性被维生素E阻断，因此其抗HCV活性可能至少部分地由ROS介导。

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《Bioorganic and Medicinal Chemistry Letters》 |2014年第17期|共5页
作者
MatsunoK.; UedaY.; FukudaM.; OnodaK.; WakiM.; IkedaM.; KatoN.; MiyachiH.;
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正文语种 eng
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Anti-HCV agent; Full genome length; HCV RNA replication; Hepatitis C virus; ORL8;

机译：抗HCV剂;全长基因组;HCV RNA复制;丙型肝炎病毒;ORL8;

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1. Synthesis and inhibitory activity on hepatitis C virus RNA replication of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxy-2-propyl)aniline analogs [J] . MatsunoK., UedaY., FukudaM., Bioorganic and Medicinal Chemistry Letters . 2014,第17期

机译：4-（1,1,1,3,3,3-六氟-2-羟基-2-丙基）苯胺类似物的丙型肝炎病毒RNA复制的合成及其抑制活性
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机译：1,4-双（1,1,1,3,3,3,3-六氟-2-羟基-2-丙基）苯的硅化和硅烷化反应
3. Fluorine-containing biochemical probes for 19{sup left}F-NMR imaging; part I: synthesis of 3,5-bis(hexafluoro-2-hydroxy-2-propyl)- and 3,5-bis(hexafluoro-2-methoxy-2-propyl)benzene derivatives having a C{sub}2v symmetry [J] . Taizp Ono, Vadim A. Soloshonok, Haruhiko Fukaya, 名古屋工業技術研究所報告 . 1996,第7期

机译：含氟生化探针19 {SUP左} F-NMR成像; 第一部分：合成3,5-双（六氟-2-羟基-2-丙基） - 和3,5-双（六氟-2-甲氧基-2-丙基）苯衍生物，具有C {} 2V对称性
4. Silencing of Hepatitis A Virus Replication by RNA Interference [C] . Y. Kusov, J. Heering, T. Kanda, European Congress of Virology . 2004

机译：通过RNA干扰沉默甲型肝炎病毒复制
5. Tizoxanide (2-hydroxy-N-(5-nitro-2-thiazolyl)benzamide) inhibits hepatitis C virus replication through modulation of NS5A hyperphosphorylation [D] . Montero, Abigail 2012

机译：噻唑烷（2-羟基-N-（5-硝基-2-噻唑基）苯甲酰胺）通过调节NS5A过度磷酸化抑制丙型肝炎病毒复制
6. Discovery of 4-(4-(2-((5-hydroxy-1234-tetrahydronaphthalen-2-yl)(propyl)amino)-ethyl)piperazin-1-yl)quinolin-8-ol and its analogues as highly potent dopamine D2/D3 agonists and as iron chelator: In vivo activity indicates potential application in symptomatic and neuroprotective therapy for Parkinson’s Disease [O] . Balaram Ghosh, Tamara Antonio, Maarten E. A. Reith, -1

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7. A Convenient Approach to the Synthesis of Deoxyribonucleoside-3′-hydrogen Phosphonates via Bis(1,1,1,3,3,3-hexafluoro-2-propyl) Phosphonate Intermediate [O] . Hiroshi Takaku, Shunitchy Yamakage, Osamu Sakatsume, 1988

机译：通过BIS（1,1,1,3,3,3-六氟-2-丙基）膦酸盐中间体合成脱氧核苷-3'-氢膦酸盐的方便方法

Synthesis and inhibitory activity on hepatitis C virus RNA replication of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxy-2-propyl)aniline analogs

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