3-(4-{6-iodoimidazo[1,2-a]pyridin-2-yl}phenyl)-1,2,4-oxadiazole | 938460-65-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-(4-{6-iodoimidazo[1,2-a]pyridin-2-yl}phenyl)-1,2,4-oxadiazole
• 英文别名: DRM102；3-[4-(6-iodoimidazo[1,2-a]pyridin-2-yl)phenyl]-1,2,4-oxadiazole
• CAS: 938460-65-2
• 化学式: C₁₅H₉IN₄O
• 分子量: 388.167
• InChiKey: YBTGUUIOJWNSLA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  56.2
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-溴-4'-氰基苯乙酮 在 盐酸羟胺 、 碳酸氢钠 、 potassium carbonate 作用下， 以 甲醇 、 乙醇 为溶剂， 反应 48.0h， 生成 3-(4-{6-iodoimidazo[1,2-a]pyridin-2-yl}phenyl)-1,2,4-oxadiazole
  参考文献：
  名称：

  Synthesis and biological evaluation of novel radioiodinated imidazopyridine derivatives for amyloid-β imaging in Alzheimer’s disease

  摘要：

  Non-invasive detection for amyloid-beta peptide (A beta) deposition has important significance for the early diagnosis and medical intervention for Alzheimer's disease (AD). In this study, we developed a series of imidazopyridine derivatives as potential imaging agents for single-photon emission computed tomography (SPECT). Two of them, compounds DRK092 and DRM106, showed higher affinity for synthetic human A beta 1-40 fibrils than did the well-known amyloid-imaging agent IMPY. A metabolite analysis revealed brain-permeable radioactive metabolites of I-125-labeled DRK092 and IMPY; no radioactive metabolites from I-125-labeled DRM106 ([I-125]DRM106) were detected. In addition, in vitro autoradiography clearly demonstrated specific binding of [I-125]DRM106 in the hippocampal region of AD enriched with A beta plaques. Thus, our results strongly suggested that compound DRM106 can be used as an imaging agent for SPECT to detect A beta deposition in AD brain. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2014.05.043

文献信息

• DIAGNOSTIC AND REMEDY FOR DISEASE CAUSED BY AMYLOID AGGREGATION AND/OR DEPOSITION
  申请人：Fujifilm RI Pharma Co., Ltd.

  公开号：EP1956013B1

  公开（公告）日：2016-04-13