6-Jod-4'-methoxy-flavon | 1033-44-9

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 黄酮类化合物
• 英文名称: 6-Jod-4'-methoxy-flavon
• 英文别名: 6-Iodo-4'-methoxyflavone；6-iodo-2-(4-methoxyphenyl)chromen-4-one
• CAS: 1033-44-9
• 化学式: C₁₆H₁₁IO₃
• 分子量: 378.166
• InChiKey: BYDBCAPACOXVEH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  35.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-Jod-4'-methoxy-flavon 在 铜 作用下， 生成 Bis-<2-(4-methoxyphenyl)-chromen-4-on-6-yl>
  参考文献：
  名称：

  化学学会会议论文集。1959年8月

  摘要：

  DOI：

  10.1039/ps9590000201
• 作为产物：
  描述：

  2-羟基-5-溴苯乙酮 在 吡啶 、 氢氧化钾 、 四(三苯基膦)钯 、 硫酸 、 六正丁基二锡 、 溶剂黄146 、 三乙胺 作用下， 以 1,4-二氧六环 为溶剂， 反应 8.0h， 生成 6-Jod-4'-methoxy-flavon
  参考文献：
  名称：

  Radioiodinated Flavones for in Vivo Imaging of β-Amyloid Plaques in the Brain

  摘要：

  In vivo imaging of beta-amyloid (A beta) peptide aggregates in the brain may lead to early detection of Alzheimer's disease (AD) and monitoring of the progression and effectiveness of AD treatment. The purpose of this study was to develop novel amyloid imaging agents based on flavone as a core structure. Radioiodinated flavone derivatives were designed and synthesized. The binding affinities of flavone derivatives for A beta aggregates varied from 13 to 77 nM. When in vitro plaque labeling was carried out using post-mortem AD brain sections, all flavones intensely stained not only amyloid plaques but also cerebrovascular amyloids. In biodistribution studies using normal mice, they displayed high brain uptakes ranging from 3.2 to 4.1% ID/g at 2 min postinjection. The radioactivity washed out from the brain rapidly (0.5-1.9% ID/g at 30 min), which is highly desirable for amyloid imaging agents. The results in the study suggest that these classes of radioiodinated flavones may be useful candidates as potential imaging agents for amyloid plaques.

  DOI：

  10.1021/jm050635e

文献信息

• Composition For Diagnosing Amyloid-Related Diseases
  申请人：Mori Hiroshi

  公开号：US20080131367A1

  公开（公告）日：2008-06-05

  A composition for diagnosing amyloid-related diseases, which comprises a flavone derivative, a chalcone derivative, a styrylchromone derivative, or a coumarin derivative, is provided. These compounds have high binding specificity to an amyloid β protein, high permeability to a blood-brain barrier, and ability to rapidly disappear from sites other than cerebral senile plaque. Accordingly, the composition of the present invention using these compounds enables the diagnosis of amyloid-related diseases with high precision.

  本发明提供了一种用于诊断淀粉样相关疾病的组合物，其中包括一种黄酮衍生物、一种查尔酮衍生物、一种苯乙烯基色酮衍生物或一种香豆素衍生物。这些化合物具有高结合特异性，能够与淀粉样β蛋白结合，具有高渗透性到血脑屏障，并能够迅速从除脑部老年斑以外的其他部位消失。因此，使用这些化合物的本发明组合物能够高精度地诊断淀粉样相关疾病。
• Composition for diagnosing amyloid-related diseases
  申请人：Nagasaki University

  公开号：US08192717B2

  公开（公告）日：2012-06-05

  A composition for diagnosing amyloid-related diseases, which comprises a flavone derivative, a chalcone derivative, a styrylchromone derivative, or a coumarin derivative, is provided. These compounds have high binding specificity to an amyloid β protein, high permeability to a blood-brain barrier, and ability to rapidly disappear from sites other than cerebral senile plaque. Accordingly, the composition of the present invention using these compounds enables the diagnosis of amyloid-related diseases with high precision.

  本发明提供了一种用于诊断淀粉样相关疾病的组合物，包括黄酮衍生物、查尔酮衍生物、苯乙烯基香豆素衍生物或香豆素衍生物。这些化合物具有高度的结合特异性，能够与淀粉样β蛋白高度结合，具有高渗透性穿过血脑屏障，且能够迅速从除老年斑外的其他部位消失。因此，使用这些化合物的本发明组合物能够高精度地诊断淀粉样相关疾病。
• COMPOSITION FOR AMYLOID-ASSOCIATED DISEASE DIAGNOSIS
  申请人：Nagasaki University

  公开号：EP1815872A1

  公开（公告）日：2007-08-08

  A composition for diagnosing amyloid-related diseases, which comprises a flavone derivative, a chalcone derivative, a styrylchromone derivative, or a coumarin derivative, is provided. These compounds have high binding specificity to an amyloid β protein, high permeability to a blood-brain barrier, and ability to rapidly disappear from sites other than cerebral senile plaque. Accordingly, the composition of the present invention using these compounds enables the diagnosis of amyloid-related diseases with high precision.

  本研究提供了一种用于诊断淀粉样蛋白相关疾病的组合物，该组合物由黄酮衍生物、查尔酮衍生物、苯乙烯基色酮衍生物或香豆素衍生物组成。 这些化合物与淀粉样β蛋白的结合特异性高，对血脑屏障的渗透性高，能够从脑衰老斑块以外的部位迅速消失。 因此，使用这些化合物的本发明组合物能够高精度地诊断淀粉样蛋白相关疾病。
• EP1815872
  申请人：——

  公开号：——

  公开（公告）日：——
• US8192717B2
  申请人：——

  公开号：US8192717B2

  公开（公告）日：2012-06-05