8-[4-[4-(dimethylamino)phenyl]triazol-1-yl]-N-hydroxyoctanamide | 1048363-70-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 8-[4-[4-(dimethylamino)phenyl]triazol-1-yl]-N-hydroxyoctanamide
• CAS: 1048363-70-7
• 化学式: C₁₈H₂₇N₅O₂
• 分子量: 345.445
• InChiKey: NJTBXOKFMYGINE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  25
• 可旋转键数：
  10
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  83.3
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  8-(4-(4-(dimethylamino)phenyl)-1H-1,2,3-triazol-1-yl)-N-(trityloxy)octanamide 在 三氟化硼乙醚 、 水 作用下， 以 甲醇 、 氯仿 为溶剂， 反应 3.0h， 以40%的产率得到8-[4-[4-(dimethylamino)phenyl]triazol-1-yl]-N-hydroxyoctanamide
  参考文献：
  名称：

  Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group

  摘要：

  Histone deacetylase inhibitors (HDACi) are endowed with plethora of biological functions including anti-proliferative, anti-inflammatory, anti-parasitic, and cognition-enhancing activities. Parsing the structure activity relationship (SAR) for each disease condition is vital for long-term therapeutic applications of HDACi. We report in the present study specific cap group substitution patterns and spacer-group chain lengths that enhance the antimalarial and antileishmanial activity of aryltriazolylhydroxamates-based HDACi. We identified many compounds that are several folds selectively cytotoxic to the plasmodium parasites compared to standard HDACi. Also, a few of these compounds have antileishmanial activity that rivals that of miltefosine, the only currently available oral agent against visceral leishmaniasis. The anti-parasite properties of several of these compounds tracked well with their anti-HDAC activities. The results presented here provide further evidence on the suitability of HDAC inhibition as a viable therapeutic option to curb infections caused by apicomplexan protozoans and trypanosomatids. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2009.10.042