1-(2-hydroxyethyl)-4-glycolyl-piperazine | 929874-81-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-(2-hydroxyethyl)-4-glycolyl-piperazine
• 英文别名: 2-Hydroxy-1-[4-(2-hydroxyethyl)piperazin-1-yl]ethanone
• CAS: 929874-81-7
• 化学式: C₈H₁₆N₂O₃
• 分子量: 188.227
• InChiKey: MLGKBQAGZVEOFZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.8
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  64
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  N-羟乙基哌嗪 、 2,2-二甲基-1,3-二氧戊环-4-酮 以 二氯甲烷 为溶剂， 以20%的产率得到1-(2-hydroxyethyl)-4-glycolyl-piperazine
  参考文献：
  名称：

  Synthesis and evaluation of in vitro anti-tuberculosis activity of N-substituted glycolamides

  摘要：

  On the basis of the structural similarity of N-substituted glycolamides with N-glycolyl muramic acid residues of the cell wall of Mycobacterium tuberculosis, a series of these compounds were designed and synthesized by the reaction of glycolic acid acetonide 1 (2,2-dimethyl-5-oxo-1,3-dioxolane) with the proper amines. The minimum inhibitory concentration (MIC) was determined against M. tuberculosis H(37)Rv in BACTEC 12B medium, using the Microplate Alamar Blue Assay (MABA). Among the synthesized compounds, all those with disubstituted amide structure accompanied by one or two heteroatom(s) with loan pair(s) of electrons atom(s) P to the amide nitrogen demonstrated moderate anti-tuberculosis activity and all the monosubstituted amides showed no activity at all. (C) 2008 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2008.02.022

文献信息

• Tyrosine kinase inhibitors
  申请人：Fraley Mark E.

  公开号：US20080274107A1

  公开（公告）日：2008-11-06

  The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

  本发明涉及抑制、调节和/或调节酪氨酸激酶信号传导的化合物，含有这些化合物的组合物，以及使用它们治疗哺乳动物中的酪氨酸激酶依赖性疾病和病状的方法，如血管生成、癌症、肿瘤生长、动脉硬化、年龄相关性黄斑变性、糖尿病视网膜病变、炎症性疾病等。
• US7186723B2
  申请人：——

  公开号：US7186723B2

  公开（公告）日：2007-03-06
• Synthesis and evaluation of in vitro anti-tuberculosis activity of N-substituted glycolamides
  作者：Fereidoon Daryaee、Farzad Kobarfard、Ali Khalaj、Parisa Farnia

  DOI：10.1016/j.ejmech.2008.02.022

  日期：2009.1

  On the basis of the structural similarity of N-substituted glycolamides with N-glycolyl muramic acid residues of the cell wall of Mycobacterium tuberculosis, a series of these compounds were designed and synthesized by the reaction of glycolic acid acetonide 1 (2,2-dimethyl-5-oxo-1,3-dioxolane) with the proper amines. The minimum inhibitory concentration (MIC) was determined against M. tuberculosis H(37)Rv in BACTEC 12B medium, using the Microplate Alamar Blue Assay (MABA). Among the synthesized compounds, all those with disubstituted amide structure accompanied by one or two heteroatom(s) with loan pair(s) of electrons atom(s) P to the amide nitrogen demonstrated moderate anti-tuberculosis activity and all the monosubstituted amides showed no activity at all. (C) 2008 Elsevier Masson SAS. All rights reserved.