5,6-dihydro-4-(2-phenylhydrazino)pyridine-2-one | 139122-77-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5,6-dihydro-4-(2-phenylhydrazino)pyridine-2-one
• 英文别名: 4-(N'-phenyl-hydrazino)-5,6-dihydro-1H-pyridin-2-one；5,6-dihydro-4-(2-phenylhydrazino)-2(1H)-pyridinone；4-(2-phenylhydrazinyl)-2,3-dihydro-1H-pyridin-6-one
• CAS: 139122-77-3
• 化学式: C₁₁H₁₃N₃O
• 分子量: 203.244
• InChiKey: LTTUVGWBUMMAME-UHFFFAOYSA-N

物化性质

• 沸点：
  335.1±42.0 °C(Predicted)
• 密度：
  1.21±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  53.2
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5,6-dihydro-4-(2-phenylhydrazino)pyridine-2-one 在 硫酸 、 lithium hexamethyldisilazane 作用下， 生成
  参考文献：
  名称：

  Selective Chemical Modulation of Gene Transcription Favors Oligodendrocyte Lineage Progression

  摘要：

  Lysine acetylation regulates gene expression through modulating protein-protein interactions in chromatin. Chemical inhibition of acetyl-lysine binding bromodomains of the major chromatin regulators BET (bromodomain and extraterminal domain) proteins has been shown to effectively block cell proliferation in cancer and inflammation. However, whether selective inhibition of individual BET bromodomains has distinctive functional consequences remains only partially understood. In this study, we show that selective chemical inhibition of the first bromodomain of BET proteins using our small-molecule inhibitor, Olinone, accelerated the progression of mouse primary oligodendrocyte progenitors toward differentiation, whereas inhibition of both bromodomains of BET proteins hindered differentiation. This effect was target specific, as it was not detected in cells treated with inactive analogs and independent of any effect on proliferation. Therefore, selective chemical modulation of individual bromodomains, rather than use of broad-based inhibitors, may enhance regenerative strategies in disorders characterized by myelin loss such as aging and neurodegeneration.

  DOI：

  10.1016/j.chembiol.2014.05.009
• 作为产物：
  描述：

  苯肼 、 2,4-哌啶二酮 在 水 作用下， 以 水 为溶剂， 反应 0.5h， 以to give title product as a light yellow solid (60 mg, yield=48%)的产率得到5,6-dihydro-4-(2-phenylhydrazino)pyridine-2-one
  参考文献：
  名称：

  INDOLONE MODULATORS OF 5-HT3 RECEPTOR

  摘要：

  本发明涉及5-HT3受体的新的吲哚酮调节剂、其药物组合物以及使用方法。

  公开号：

  US20100113478A1

文献信息

• [EN] SMALL MOLECULE TRANSCRIPTION MODULATORS OF BROMODOMAINS<br/>[FR] MODULATEURS DE LA TRANSCRIPTION DE PETITE MOLÉCULE DE BROMODOMAINES
  申请人：ICAHN SCHOOL MED MOUNT SINAI

  公开号：WO2015184257A3

  公开（公告）日：2016-01-21
• Process for the preparation of lactam derivatives
  申请人：GLAXO GROUP LIMITED

  公开号：EP0458624B1

  公开（公告）日：1998-04-01
• Small Molecule Transcription Modulators of Bromodomains
  申请人：Icahn School of Medicine at Mount Sinai

  公开号：US20170107218A1

  公开（公告）日：2017-04-20

  This disclosure relates generally to compounds and compositions comprising one or more indole analogs. These compounds are useful for treating diseases associated with NF-kB and p53 activity, such as cancer and inflammatory diseases.
• US5196534A
  申请人：——

  公开号：US5196534A

  公开（公告）日：1993-03-23