| 1088496-51-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• CAS: 1088496-51-8
• 化学式: C₁₄H₁₆ClNO₄
• 分子量: 297.738
• InChiKey: YWMJQLAUDMNMBF-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  、 间溴苯胺 以 二氯甲烷 为溶剂， 生成
  参考文献：
  名称：

  Optimization and structure–activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: Identification of MK-0873, a potent and effective PDE4 inhibitor

  摘要：

  A SAR study of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides is described. Optimization of the series was based on in vitro potency against PDE4, inhibition of the LPS-induced production of TNF-alpha in human whole blood and minimizing affinity for the hERG potassium channel. From these studies, compounds 18 and 20 (MK-0873) were identified as optimized PDE4 inhibitors with good overall in vitro and in vivo profiles and selected as development candidates. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.09.009
• 作为产物：
  描述：

  ethyl 3-(2-chloro-6-methyl(3-pyridyl))-3-oxopropanoate 、 原甲酸三乙酯 在 乙酸酐 作用下， 生成
  参考文献：
  名称：

  Optimization and structure–activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: Identification of MK-0873, a potent and effective PDE4 inhibitor

  摘要：

  A SAR study of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides is described. Optimization of the series was based on in vitro potency against PDE4, inhibition of the LPS-induced production of TNF-alpha in human whole blood and minimizing affinity for the hERG potassium channel. From these studies, compounds 18 and 20 (MK-0873) were identified as optimized PDE4 inhibitors with good overall in vitro and in vivo profiles and selected as development candidates. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.09.009