| 570398-81-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• CAS: 570398-81-1
• 化学式: C₂₆H₃₁N₃O₃
• 分子量: 433.55
• InChiKey: QZVJQUIJOZDVRG-DEOSSOPVSA-N

反应信息

• 作为反应物：
  描述：

  在 ammonium cerium (IV) nitrate 作用下， 以 水 、 乙腈 为溶剂， 生成
  参考文献：
  名称：

  Oxygenated analogues of UK-396082 as inhibitors of activated thrombin activatable fibrinolysis inhibitor

  摘要：

  A suitable inhibitor of activated thrombin activatable. brinolysis inhibitor (TAFIa) has the potential to be a novel treatment for thrombosis. The TAFIa inhibitor UK-396082 (1) was used as a starting point to seek more potent analogues. With knowledge of encouraging human pharmacokinetics and toleration for the clinical candidate (1), the programme continued to seek structure-activity relationships (SAR) that could positively impact on both potency and half-life, and therefore the projected dose of any future nominated clinical agent. A series of oxygenated analogues based on compound 1 were prepared to evaluate changes in pharmacology, selectivity and pharmacokinetics. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.11.029
• 作为产物：
  描述：

  生成 、
  参考文献：
  名称：

  Oxygenated analogues of UK-396082 as inhibitors of activated thrombin activatable fibrinolysis inhibitor

  摘要：

  A suitable inhibitor of activated thrombin activatable. brinolysis inhibitor (TAFIa) has the potential to be a novel treatment for thrombosis. The TAFIa inhibitor UK-396082 (1) was used as a starting point to seek more potent analogues. With knowledge of encouraging human pharmacokinetics and toleration for the clinical candidate (1), the programme continued to seek structure-activity relationships (SAR) that could positively impact on both potency and half-life, and therefore the projected dose of any future nominated clinical agent. A series of oxygenated analogues based on compound 1 were prepared to evaluate changes in pharmacology, selectivity and pharmacokinetics. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.11.029