6-amino-2-(furan-2-yl)-3-hydroxy-4H-chromen-4-one | 1060132-24-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: 6-amino-2-(furan-2-yl)-3-hydroxy-4H-chromen-4-one
• 英文别名: 6-amino-2-(2-furanyl)-3-hydroxy-4H-1-benzopyran-4-one；6-amino-2-(furan-2-yl)-3-hydroxychromen-4-one
• CAS: 1060132-24-2
• 化学式: C₁₃H₉NO₄
• 分子量: 243.219
• InChiKey: FEFOJBCAHQLHBY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  18
• 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：
  85.7
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  马来酸酐 、 6-amino-2-(furan-2-yl)-3-hydroxy-4H-chromen-4-one 在 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以90%的产率得到4-[[2-(2-furanyl)-3-hydroxy-4-oxo-4H-1-benzopyran-6-yl]amino]-4-oxo-2-butenoic acid
  参考文献：
  名称：

  Fluorescent Ratiometric MFC Probe Sensitive to Early Stages of α-Synuclein Aggregation

  摘要：

  We introduce a sensor molecule, AS140-MFC, consisting of a covalent adduct of an Ala-to-Cys mutant of alpha-synuclein with the 3-hydroxychromone dual emission dye MFC. We show that the AS140-MFC construct is a multiparametric fluorescent probe suitable for the continuous monitoring of protein aggregation and is sensitive to the early and intermediate stages of alpha-synuclein aggregation, a process associated with Parkinson's disease.

  DOI：

  10.1021/ja102838n
• 作为产物：
  描述：

  N-(2-(furan-2-yl)-3-hydroxy-4-oxo-4H-chromen-6-yl)acetamide 在 盐酸 、 水 作用下， 以 乙醇 为溶剂， 反应 7.0h， 以90%的产率得到6-amino-2-(furan-2-yl)-3-hydroxy-4H-chromen-4-one
  参考文献：
  名称：

  Fluorescent Ratiometric MFC Probe Sensitive to Early Stages of α-Synuclein Aggregation

  摘要：

  We introduce a sensor molecule, AS140-MFC, consisting of a covalent adduct of an Ala-to-Cys mutant of alpha-synuclein with the 3-hydroxychromone dual emission dye MFC. We show that the AS140-MFC construct is a multiparametric fluorescent probe suitable for the continuous monitoring of protein aggregation and is sensitive to the early and intermediate stages of alpha-synuclein aggregation, a process associated with Parkinson's disease.

  DOI：

  10.1021/ja102838n

文献信息

• [EN] COMPOUNDS FOR THE TREATMENT OF AMYLOID-ASSOCIATED DISEASES<br/>[FR] COMPOSÉS POUR LE TRAITEMENT DE MALADIES ASSOCIÉES À LA SUBSTANCE AMYLOÏDE
  申请人：REMYND NV

  公开号：WO2016083490A1

  公开（公告）日：2016-06-02

  This invention provides novel compounds of formulae (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein the substituents are as defined in the specification. The present invention also relates to the novel compounds for use as a medicine, more in particular for the prevention or treatment of amyloid-related diseases, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such amyloid-related diseases. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

  这项发明提供了式(I)或(II)或其立体异构体、对映异构体、消旋体或互变异构体的新化合物，其中取代基如规范中所定义。本发明还涉及用作药物的这些新化合物，更具体地用于预防或治疗与淀粉样蛋白相关的疾病，更具体地说是某些神经系统疾病，如被统称为tau病变的疾病，以及由细胞毒性α-突触核蛋白淀粉生成所特征化的疾病。本发明还涉及利用这些新化合物制备对治疗此类淀粉样蛋白相关疾病有用的药物。本发明还涉及包括这些新化合物的药物组合物以及这些新化合物的制备方法。