1-methoxy-4-[(4-methoxyphenyl)sulfonyl]naphthalene

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 1-methoxy-4-[(4-methoxyphenyl)sulfonyl]naphthalene
• 英文别名: 4-Methoxyphenyl 4-methoxy-1-naphthyl sulfone；1-methoxy-4-(4-methoxyphenyl)sulfonylnaphthalene
• 化学式: C₁₈H₁₆O₄S
• 分子量: 328.389
• InChiKey: NLDCUXHIAKMEBJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  61
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-methoxy-4-[(4-methoxyphenyl)sulfonyl]naphthalene 在 三溴化硼 、 水 作用下， 以 二氯甲烷 为溶剂， 反应 20.3h， 以58%的产率得到4-[(4-methoxyphenyl)sulfonyl]naphthol
  参考文献：
  名称：

  Design, Synthesis, and Structure–Activity Relationship of N-Arylnaphthylamine Derivatives as Amyloid Aggregation Inhibitors

  摘要：

  Dyes like CR are able to inhibit the aggregation of A beta fibrils. Thus, a screening of a series of dyes including ABBB (1) was performed. Its main component 2 tested in an in vitro assay (i.e., ThT assay) showed good potency at inhibiting fibrils association. Congeners 4-9 have been designed and synthesized as inhibitors of A beta aggregation. A nurnber of these newly synthesized compounds have been found to be active in the ThT assay with IC50 of 1-57.4 mu M. The most potent compound of this series, 4k, showed micromolar activity in this test. Another potent derivative 4q (IC50 = 5.6 mu M) rapidly crossed the blood-brain barrier, achieving whole brain concentrations higher than in plasma. So 4q could be developed to find novel potent antiaggregating beta A agents useful in Alzheimer disease as well as other neurological diseases characterized by deposits of amyloid aggregates.

  DOI：

  10.1021/jm301105m
• 作为产物：
  描述：

  1-碘-4-甲氧基萘 在 tris-(dibenzylideneacetone)dipalladium(0) 、 potassium peroxymonosulfate 、 potassium tert-butylate 、 双(2-二苯基磷苯基)醚 作用下， 以 甲醇 、 水 、 甲苯 为溶剂， 反应 18.0h， 生成 1-methoxy-4-[(4-methoxyphenyl)sulfonyl]naphthalene
  参考文献：
  名称：

  Design, Synthesis, and Structure–Activity Relationship of N-Arylnaphthylamine Derivatives as Amyloid Aggregation Inhibitors

  摘要：

  Dyes like CR are able to inhibit the aggregation of A beta fibrils. Thus, a screening of a series of dyes including ABBB (1) was performed. Its main component 2 tested in an in vitro assay (i.e., ThT assay) showed good potency at inhibiting fibrils association. Congeners 4-9 have been designed and synthesized as inhibitors of A beta aggregation. A nurnber of these newly synthesized compounds have been found to be active in the ThT assay with IC50 of 1-57.4 mu M. The most potent compound of this series, 4k, showed micromolar activity in this test. Another potent derivative 4q (IC50 = 5.6 mu M) rapidly crossed the blood-brain barrier, achieving whole brain concentrations higher than in plasma. So 4q could be developed to find novel potent antiaggregating beta A agents useful in Alzheimer disease as well as other neurological diseases characterized by deposits of amyloid aggregates.

  DOI：

  10.1021/jm301105m

文献信息

• Dissymmetric new polymer materials
  申请人：Shell Oil Company

  公开号：US04960912A1

  公开（公告）日：1990-10-02

  Dissymmetric new epoxy polymer materials have improved process-ability because they can be cured at lower temperatures.

  非对称的新环氧聚合物材料由于可以在较低温度下固化，因此具有改善的加工性能。
• Dissymmetric polymer materials
  申请人：Shell Oil Company

  公开号：US04996279A1

  公开（公告）日：1991-02-26

  Dissymmetric new epoxy polymer materials have improved processability because they can be cured at lower temperatures.

  不对称的新环氧聚合物材料具有改进的加工性能，因为它们可以在较低的温度下固化。
• Naphthyl Derivatives as Inhibitors of Beta-Amyloid Aggregation
  申请人：Minetti Patrizia

  公开号：US20080255232A1

  公开（公告）日：2008-10-16

  Compounds useful in the treatment of disorders characterized by deposits of amyloid aggregates are herein described together with pharmaceutical compounds containing the same. In particular the compounds of the present invention are those having the Formula (I) as reported below, where the radicals have the meaning indicated in the description.

  本文描述了用于治疗由淀粉样聚集物沉积所特征化的疾病的化合物，以及含有相同化合物的药物化合物。特别是，本发明的化合物是具有下面报告的式（I）的化合物，其中基团具有描述中所示的含义。
• WO2007/45593
  申请人：——

  公开号：——

  公开（公告）日：——
• NAPHTHYL DERIVATIVES AS INHIBITORS OF BETA-AMYLOID AGGREGATION
  申请人：SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.

  公开号：EP1937243A2

  公开（公告）日：2008-07-02