2-((4-fluorobenzyl)sulfonyl)-4-(4-fluorophenyl)-1-methyl-1H-imidazole | 1443114-32-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-((4-fluorobenzyl)sulfonyl)-4-(4-fluorophenyl)-1-methyl-1H-imidazole
• CAS: 1443114-32-6
• 化学式: C₁₇H₁₄F₂N₂O₂S
• 分子量: 348.373
• InChiKey: VMPVYFXLSALWTF-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  2-((4-fluorobenzyl)sulfonyl)-4-(4-fluorophenyl)-1-methyl-1H-imidazole 在 N-溴代丁二酰亚胺(NBS) 作用下， 以 四氯化碳 为溶剂， 以80%的产率得到5-bromo-2-((4-fluorobenzyl)sulfonyl)-4-(4-fluorophenyl)-1-methyl-1H-imidazole
  参考文献：
  名称：

  Synthesis and Metabolic Studies of Host-Directed Inhibitors for Antiviral Therapy

  摘要：

  Targeting host cell factors required for virus replication provides an alternative to targeting pathogen components and represents a promising approach to develop broad-spectrum antiviral therapeutics. High-throughput screening (HTS) identified two classes of inhibitors (2 and 3) with broad-spectrum antiviral activity against ortho- and paramyxoviruses including influenza A virus (IAV), measles virus (MeV), respiratory syncytial virus (RSV), and human parainfluenza virus type 3 (HPIV3). Hit-to-lead optimization delivered inhibitor 28a, with EC50 values of 0.88 and 0.81 mu M against IAV strain WSN and MeV strain Edmonston, respectively. It was also found that compound 28a delivers good stability in human liver S9 fractions with a half-life of 165 min. These data establish 28a as a promising lead for antiviral therapy through a host-directed mechanism.

  DOI：

  10.1021/ml400166b
• 作为产物：
  描述：

  2-((4-fluorobenzyl)thio)-4-(4-fluorophenyl)-1-methyl-1H-imidazole 在 双氧水 作用下， 以 溶剂黄146 为溶剂， 以69%的产率得到2-((4-fluorobenzyl)sulfonyl)-4-(4-fluorophenyl)-1-methyl-1H-imidazole
  参考文献：
  名称：

  Synthesis and Metabolic Studies of Host-Directed Inhibitors for Antiviral Therapy

  摘要：

  Targeting host cell factors required for virus replication provides an alternative to targeting pathogen components and represents a promising approach to develop broad-spectrum antiviral therapeutics. High-throughput screening (HTS) identified two classes of inhibitors (2 and 3) with broad-spectrum antiviral activity against ortho- and paramyxoviruses including influenza A virus (IAV), measles virus (MeV), respiratory syncytial virus (RSV), and human parainfluenza virus type 3 (HPIV3). Hit-to-lead optimization delivered inhibitor 28a, with EC50 values of 0.88 and 0.81 mu M against IAV strain WSN and MeV strain Edmonston, respectively. It was also found that compound 28a delivers good stability in human liver S9 fractions with a half-life of 165 min. These data establish 28a as a promising lead for antiviral therapy through a host-directed mechanism.

  DOI：

  10.1021/ml400166b