(E,E)-3,5-bis-(4'-hydroxystyryl)phenol | 1202470-74-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二芳基庚烷
• 英文名称: (E,E)-3,5-bis-(4'-hydroxystyryl)phenol
• 英文别名: (E,E)-3,5-bis(4'-hydroxystyryl)phenol；3,5-bis[(E)-2-(4-hydroxyphenyl)vinyl]phenol；3,5-bis[(E)-2-(4-hydroxyphenyl)ethenyl]phenol
• CAS: 1202470-74-3
• 化学式: C₂₂H₁₈O₃
• 分子量: 330.383
• InChiKey: ICUPUOLNNGGWKO-ZPUQHVIOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  60.7
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (E,E)-3,5-bis(4'-methoxymethoxystyryl)phenol 在 盐酸 作用下， 以 乙醇 、 水 为溶剂， 以94%的产率得到(E,E)-3,5-bis-(4'-hydroxystyryl)phenol
  参考文献：
  名称：

  Small molecules that protect against β-amyloid-induced cytotoxicity by inhibiting aggregation of β-amyloid

  摘要：

  Aggregated beta-amyloid (A beta) plays crucial roles in Alzheimer's disease (AD) pathogenesis, therefore blockade of Ab aggregation is considered as a potential therapeutic target. We designed and synthesized small molecules to reduce A beta-induced cytotoxicity by inhibiting A beta aggregation. The small molecules were screened via ThT, MTT, and cell-based cytotoxicity assay (A beta burden assay). Selected compounds 1c, 1d, 1e, and 1f were then investigated by evaluating their effects on cognitive impairment of acute AD mice model. Learning and memory dysfunction by injection of A beta(1-42) was recovered by administration of these molecules. Especially, 1d showed the best recovery activity in Y-maze task, object recognition task, and passive avoidance task with dose dependent manner. These results suggest that 1d has high potential as a therapeutic agent for AD. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2012.06.045

文献信息

• BIS(STYRYL)PYRIMIDINE OR BIS(STYRYL)BENZENE COMPOUNDS, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF DISEASES FEATURING AMYLOIDS COMPRISING THE SAME AS AN ACTIVE INGREDIENT
  申请人：SHIN Kye Jung

  公开号：US20100190803A1

  公开（公告）日：2010-07-29

  Disclosed are bis(styryl)pyrimidine or bis(styryl)benzene compounds, represented by Chemical Formula 1, pharmaceutically acceptable salts, a method for preparing the same, and a pharmaceutical composition for the prevention and treatment of amyloidosis-associated diseases, comprising the same as an active ingredient. Having the ability to inhibit the deposition of beta amyloid and to reduce the toxicity of beta amyloid, the derivatives can improve learning and memory and can be useful in the prevention and treatment of amyloidosis-associated diseases. (wherein R 1 , R 2 , R 3 and X are as defined in the specification)

  本发明涉及一种由化学式1表示的双(苯乙烯基)嘧啶或双(苯乙烯基)苯化合物，其药学上可接受的盐，其制备方法以及一种药物组合物，用于预防和治疗与淀粉样蛋白病相关的疾病，其中该化合物为活性成分。该衍生物具有抑制β淀粉样蛋白沉积和减少其毒性的能力，可以改善学习和记忆，并且可以在预防和治疗与淀粉样蛋白病相关的疾病方面有用。（其中R1、R2、R3和X如规范中所定义）
• [EN] PROCESS FOR THE MANUFACTURE OF HYDROXY-SUBSTITUTED AROMATIC COMPOUNDS<br/>[FR] PROCÉDÉ DE FABRICATION DE COMPOSÉS AROMATIQUES HYDROXY-SUBSTITUÉS
  申请人：BASF SE

  公开号：WO2017194590A1

  公开（公告）日：2017-11-16

  The present invention relates to a process for the manufacture of hydroxy-substituted aromatic styryl or stilbene compounds.

  本发明涉及一种制备羟基取代的芳香基苯乙烯或苯乙烯化合物的过程。
• Shunt delivery of curcumin for the treatment Alzneimer
  申请人：Codman & Shurtleff, Inc.

  公开号：EP2359820A1

  公开（公告）日：2011-08-24

  A method for reducing or preventing a human brain disorder relating to the presence of a pathogenic substance in cerebrospinal fluid by selecting a human for treatment as a patient and placing a proximal end of a first catheter, having at least a first lumen, in a first sub-dural location within the brain of the patient to establish open communication between the first lumen and cerebrospinal fluid of the patient. For an extended period of time, a curcumin agent selected from at least one of curcumin, a curcumin hybrid and a curcumin analog is delivered to the cerebrospinal fluid to interact with the pathogenic substance to attenuate its effect on the brain.

  一种减少或预防与脑脊液中存在致病物质有关的人类脑部疾病的方法，其方法是选择人类作为患者进行治疗，并将具有至少第一管腔的第一导管的近端置于患者脑内的第一硬膜下位置，以建立第一管腔与患者脑脊液之间的开放式交流。在一段较长的时间内，选自姜黄素、姜黄素混合物和姜黄素类似物中至少一种的姜黄素制剂被输送到脑脊液中，与致病物质相互作用，以减弱其对大脑的影响。
• Curcumin-resveratrol hybrids
  申请人：Codman & Shurtleff, Inc.

  公开号：EP2749552A1

  公开（公告）日：2014-07-02

  Novel molecules based upon hybridization of curcumin and hydroxystilbenes, such as resveratrol. It is believed that these novel molecules will have special application in treating Alzheimer's disease.

  基于姜黄素和羟基二苯乙烯（如白藜芦醇）杂交的新型分子。相信这些新型分子在治疗阿尔茨海默氏症方面会有特殊用途。
• USE OF NITROGEN-CONTAINING CURCUMIN ANALOGS FOR THE TREATMENT ALZHEIMER'S DISEASE
  申请人：Codman & Shurtleff, Inc.

  公开号：EP2382176A1

  公开（公告）日：2011-11-02