2-(4-aminophenyl)indolizine | 139705-73-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯
• 英文名称: 2-(4-aminophenyl)indolizine
• 英文别名: 4-indolizin-2-yl-aniline；4-Indolizin-2-yl-anilin；4-indolizin-2-ylaniline
• CAS: 139705-73-0
• 化学式: C₁₄H₁₂N₂
• 分子量: 208.263
• InChiKey: FCAVXOBTHSDVQN-UHFFFAOYSA-N

物化性质

• 密度：
  1.15±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  30.4
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2-(4-aminophenyl)indolizine 生成 sulfanilic acid-(4-indolizin-2-yl-anilide)
  参考文献：
  名称：

  Buu-Hoi; Khoi, Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, 1950, vol. 230, p. 967

  摘要：

  DOI：
• 作为产物：
  描述：

  2-溴-1-(4-硝基苯基)乙醇 在 乙醇 、 tin(ll) chloride 作用下， 生成 2-(4-aminophenyl)indolizine
  参考文献：
  名称：

  Buu-Hoi; Khoi, Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, 1950, vol. 230, p. 967

  摘要：

  DOI：

文献信息

• Bioreductive fluorescent markers for hypoxic cells: a study of 2-nitroimidazoles with 1-substituents containing fluorescent, bridgehead-nitrogen, bicyclic systems
  作者：Richard J. Hodgkiss、Richard W. Middleton、John Parrick、Harshad K. Rami、Peter Wardman、George D. Wilson

  DOI：10.1021/jm00088a030

  日期：1992.5

  cells was compared by flow cytometric analysis. A wide range of cellular fluorescence and hypoxic-oxic differentials in fluorescence was observed when compounds with indolizine fluorophors were incubated with cells, and one such compound was considered suitable for further evaluation in vivo. Two compounds with bimane fluorophors gave very little cellular fluorescence when incubated with hypoxic cells

  用荧光侧链标记的2-硝基咪唑的氧敏感性生物还原结合已用于选择性染色低氧哺乳动物细胞。用含有具有桥头氮原子的荧光双环体系的1-取代基合成了几种新型化合物。荧光团与硝基咪唑之间的连接中还包括其他胺和仲醇取代基，以改善水溶性。通过流式细胞术分析比较了它们区分低氧和氧细胞的能力。当将带有吲哚嗪荧光团的化合物与细胞一起孵育时，观察到了范围广泛的细胞荧光和低氧-氧差异，并且认为其中一种这样的化合物适合于体内进一步评估。
• Imaging Agents Useful for Identifying AD Pathology
  申请人：Kolb Hartmuth C.

  公开号：US20100098634A1

  公开（公告）日：2010-04-22

  Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.

  本文提供的化合物和组合物包含如下所述的公式，其中该化合物是一种淀粉样蛋白结合化合物。本发明的淀粉样蛋白结合化合物可以以适量的方式用于体内成像淀粉样沉积物，以区分含有淀粉样沉积物的神经组织和正常神经组织。本发明的淀粉样探针可以用于检测和定量测量包括唐氏综合症、家族性阿尔茨海默病在内的疾病中的淀粉样沉积物。在另一实施例中，这些化合物可以用于治疗或预防神经退行性疾病。本文还提供了一种使化合物分布到脑组织中并成像脑组织的方法，其中与正常结合水平相比，化合物与脑组织的结合增加表明哺乳动物正在患有或有发展神经退行性疾病的风险。
• Imaging agents useful for identifying AD pathology
  申请人：Kolb Hartmuth C.

  公开号：US08420052B2

  公开（公告）日：2013-04-16

  Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.

  本文提供了包含所述配方的化合物和组合物，其中该化合物是一种淀粉样蛋白结合化合物。根据本发明，可以将淀粉样蛋白结合化合物以适当的剂量用于体内成像淀粉样沉积物，并区分带有淀粉样沉积物和正常神经组织的神经组织。本发明的淀粉样探针可用于检测和定量测定包括唐氏综合症、家族性阿尔茨海默病等疾病中的淀粉样沉积物。在另一实施方案中，这些化合物可用于治疗或预防神经退行性疾病。本文还提供了一种使化合物分布到脑组织中并成像脑组织的方法，其中与正常结合水平相比，化合物与脑组织的结合增加表明哺乳动物正在患有或有发展神经退行性疾病的风险。
• IMAGING AGENTS USEFUL FOR IDENTIFYING AD PATHOLOGY
  申请人：Siemens Medical Solutions USA, Inc.

  公开号：EP2323697A2

  公开（公告）日：2011-05-25
• US8420052B2
  申请人：——

  公开号：US8420052B2

  公开（公告）日：2013-04-16