2-Methyl-2,4-bis(2-nitrophenyl)-1,3-dihydro-1,5-benzodiazepine | 1235974-13-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 英文名称: 2-Methyl-2,4-bis(2-nitrophenyl)-1,3-dihydro-1,5-benzodiazepine
• CAS: 1235974-13-6
• 化学式: C₂₂H₁₈N₄O₄
• 分子量: 402.409
• InChiKey: JMJRGERCOBNCCF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  30
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  116
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  邻硝基苯乙酮 、 邻苯二胺 在 silica gel-supported sulfuric acid 作用下， 以 甲醇 为溶剂， 反应 0.83h， 以95%的产率得到2-Methyl-2,4-bis(2-nitrophenyl)-1,3-dihydro-1,5-benzodiazepine
  参考文献：
  名称：

  Anti-neuroinflammatory activity of 1,5-benzodiazepine derivatives

  摘要：

  A series of 2,3-dihydro-1,5-benzodiazepines were synthesized and evaluated for anti-inflammatory effects in microglia cells. Among the 1,5-benzodiazepines tested, compound 3e strongly inhibited LPS-induced nitric oxide ( NO) production, with an IC50 value of 7.0 mu M in the microglia cells. Also, compound 3e significantly inhibited the enzymatic activity of inducible NO synthase ( iNOS) without changes in iNOS protein expression or NO scavenging activity. This result suggests that compound 3e showed anti-neuroinflammatory effects by suppressing iNOS enzyme activity. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.04.133

文献信息

• Anti-neuroinflammatory activity of 1,5-benzodiazepine derivatives
  作者：Sang Keun Ha、Donthabhaktuni Shobha、Eunjung Moon、Murugulla A. Chari、Kagga Mukkanti、Sung-Hoon Kim、Kwang-Hyun Ahn、Sun Yeou Kim

  DOI：10.1016/j.bmcl.2010.04.133

  日期：2010.7

  A series of 2,3-dihydro-1,5-benzodiazepines were synthesized and evaluated for anti-inflammatory effects in microglia cells. Among the 1,5-benzodiazepines tested, compound 3e strongly inhibited LPS-induced nitric oxide ( NO) production, with an IC50 value of 7.0 mu M in the microglia cells. Also, compound 3e significantly inhibited the enzymatic activity of inducible NO synthase ( iNOS) without changes in iNOS protein expression or NO scavenging activity. This result suggests that compound 3e showed anti-neuroinflammatory effects by suppressing iNOS enzyme activity. (C) 2010 Elsevier Ltd. All rights reserved.