| 1174986-63-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• CAS: 1174986-63-0
• 化学式: C₁₄H₁₃NO₄
• 分子量: 259.262
• InChiKey: AROOGJNAMDWUMB-CMDGGOBGSA-N

反应信息

• 作为产物：
  描述：

  在 水 、 potassium hydroxide 作用下， 以 乙醇 为溶剂， 反应 1.0h， 生成
  参考文献：
  名称：

  Structure–activity relationships of heteroaromatic esters as human rhinovirus 3C protease inhibitors

  摘要：

  Human rhinovirus 3C protease (HRV 3C(pro)) is known to be a promising target for development of therapeutic agents against the common cold because of the importance of the protease in viral replication as well as its expression in a large number of serotypes. To explore non-peptidic inhibitors of HRV 3C(pro), a series of novel heteroaromatic esters was synthesized and evaluated for inhibitory activity against HRV 3C(pro), to determine the structure-activity relationships. The most potent inhibitor, 7, with a 5-bromopyridinyl group, had an IC50 value of 80 nM. In addition, the binding mode of a novel analog, 19, with the 4-hydroxyquinolinone moiety, was explored by molecular docking, suggesting a new interaction in the S1 pocket. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.04.114