| 1041007-69-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• CAS: 1041007-69-5
• 化学式: C₃H₆N₂O₄
• 分子量: 136.078
• InChiKey: PZFQKMJVRDKVMJ-MQIHXRCWSA-N

反应信息

• 作为产物：
  描述：

  丙二酸二乙酯 在 ¹⁵N-hydroxylamine 、 sodium methylate 作用下， 以 甲醇 、 水 为溶剂， 生成
  参考文献：
  名称：

  Hydroxamic Acids As a Novel Family of Serine Racemase Inhibitors: Mechanistic Analysis Reveals Different Modes of Interaction with the Pyridoxal-5′-phosphate Cofactor

  摘要：

  Mammalian serine racemase (SR) is a pyridoxal-5-phosphate (PLP) dependent enzyme responsible for the biosynthesis of the neurotransmitter D-Scrine, which activates N-methyl-D-aspartate (NMDA) receptors in the CNS. Aberrant regulation of NMDA receptor signaling has been implicated in a variety of neuropathologies, and inhibitors of SR would therefore be a worthwhile too] for further investigation or treatment of such conditions. Here, we identify a series of small aliphatic hydroxamic acids (HAS) that act as potent SR inhibitors. However, specificity studies showed that some of these HAS can act as nonspecific inhibitors of PLP-dependent enzymes. We employed NMR, MS, and UV/vis spectroscopic techniques to reveal that the nonspecific effect is likely due to irreversible interaction of the HA moiety with PLP to form aldoxime species. We also characterize L-aspartic acid beta-hydroxamate as a competitive and selective SR inhibitor that could be used as a scaffold for further inhibitor development.

  DOI：

  10.1021/jm900775q