5-(2-氨基-1-(4-吗啉基苯基)-1H-苯并咪唑-6-基)-N-(2-氟苯基)-2-甲氧基吡啶-3-磺酰胺 | 1416334-69-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 中文名称: 5-(2-氨基-1-(4-吗啉基苯基)-1H-苯并咪唑-6-基)-N-(2-氟苯基)-2-甲氧基吡啶-3-磺酰胺
• 英文名称: 5-(2-amino-1-(4-morpholinophenyl)-1H-benzo[d]imidazol-6-yl)-N-(2-fluorophenyl)-2-methoxypyridine-3-sulfonamide
• 英文别名: 5-[2-amino-3-(4-morpholin-4-ylphenyl)benzimidazol-5-yl]-N-(2-fluorophenyl)-2-methoxypyridine-3-sulfonamide
• CAS: 1416334-69-4
• 化学式: C₂₉H₂₇FN₆O₄S
• 分子量: 574.636
• InChiKey: AJOGHKUZDLYXKS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  41
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  133
• 氢给体数：
  2
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  4-(4-吗啉基)苯胺 在 1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物 sodium dithionite 、 potassium acetate 、 potassium carbonate 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 甲醇 、 水 、 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 反应 8.67h， 生成 5-(2-氨基-1-(4-吗啉基苯基)-1H-苯并咪唑-6-基)-N-(2-氟苯基)-2-甲氧基吡啶-3-磺酰胺
  参考文献：
  名称：

  [EN] BENZIMIDAZOLE DERIVATIVES AS ANTIVIRAL AGENTS
  [FR] DÉRIVÉS DE BENZIMIDAZOLE EN TANT QU'AGENTS ANTIVIRAUX

  摘要：

  公开号：

  WO2012174312A3

文献信息

• Method for screening drug and therapeutic targets used for treating Alzheimer's disease
  申请人：Jiangsu Nuo-Beta Pharmaceutical Technology Co., Ltd.

  公开号：US11236378B2

  公开（公告）日：2022-02-01

  Disclosed is the use of genetic means or a related inhibitor to inhibit and down-regulate the amount of PI4KIIIα protein, RBO/EFR3/EFR3A/EFR3B membrane proteins, TTC7 protein and membrane protein complexes formed by said proteins, or related enzyme activity to promote Aβ secretion by neuronal cells, reduce Aβ accumulation within neurons, and thereby reduce AD model fruit fly and mouse nerve dysfunction.

  所公开的是利用遗传手段或相关抑制剂来抑制和下调 PI4KIIIα 蛋白、RBO/EFR3/EFR3A/EFR3B 膜蛋白、TTC7 蛋白和由上述蛋白形成的膜蛋白复合物或相关酶活性的数量，以促进神经元细胞分泌 Aβ，减少 Aβ 在神经元内的积累，从而减轻 AD 模型果蝇和小鼠的神经功能障碍。
• Method For Screening Drug And Therapeutic Targets Used For Treating Alzheimer's Disease
  申请人：Jiangsu Nuo-Beta Pharmaceutical Technology Co., Ltd.

  公开号：US20190211371A1

  公开（公告）日：2019-07-11

  Disclosed is the use of genetic means or a related inhibitor to inhibit and down-regulate the amount of PI4KIIIα protein, RBO/EFR3/EFR3A/EFR3B membrane proteins, TTC7 protein and membrane protein complexes formed by said proteins, or related enzyme activity to promote Aβ secretion by neuronal cells, reduce Aβ accumulation within neurons, and thereby reduce AD model fruit fly and mouse nerve dysfunction.
• Application Of PI4KIIIA Protein And Related Membrane Protein Complex In Treating Alzheimer's Disease
  申请人：Jiangsu Nuo-Beta Pharmaceutical Technology Co. Ltd.

  公开号：US20190314321A1

  公开（公告）日：2019-10-17

  The use of a genetic method to down-regulate RBO/EFR3/EFR3A/EFR3B proteins, TTC7 protein or PI4KIIIα enzyme protein which interacts with RBO/EFR3/EFR3A/EFR3B proteins and TTC7 protein, or the use of a drug to inhibit PI4KIIIα protein kinase activity reduces the accumulation of Aβ 42 within neurons and age-dependent synaptic transmission failure and other obstacles in a fruit fly AD model, and obtains an effect of improving the learning and memory abilities of AD model mice. Provided is a method for using an RBO/EFR3/EFR3A/EFR3B inhibitor, a TTC7 inhibitor and a PI4KIIIα inhibitor to treat Alzheimer's disease. Also provided is a method for screening a drug treating Alzheimer's disease by whether Aβ secretion by nerve cells is promoted or not.