1-(5-Phenyl-2,3-dihydro-1,3,4-thiadiazol-2-yl)naphthalen-2-ol

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 1-(5-Phenyl-2,3-dihydro-1,3,4-thiadiazol-2-yl)naphthalen-2-ol
• 化学式: C₁₈H₁₄N₂OS
• 分子量: 306.4
• InChiKey: QIHMPEZAXBQNBF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  69.9
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Agents for reversing epigenetic silencing of genes
  申请人：The Johns Hopkins University

  公开号：US10227654B2

  公开（公告）日：2019-03-12

  The present invention provides methods for discovering agents that are effective in reversing epigenetic silencing by inhibiting the interaction of methyl-binding (MBD) proteins with methylated genomic DNA. Also provided are methods for reactivating silenced genes having CpG island hypermethylation along with methods for treatment and prevention of diseases, such as cancer and sickle cell anemia, by administering an agent that modulates methyl-binding domain (MBD) protein-mediated transcriptional repression, thereby increasing gene transcription to prevent or treat disease. Additionally, compounds identified by the present invention useful for treatment and prevention of diseases, such as cancer and sickle cell anemia, are provided.

  本发明提供了通过抑制甲基结合（MBD）蛋白与甲基化基因组 DNA 的相互作用，发现可有效逆转表观遗传沉默的制剂的方法。本发明还提供了重新激活具有 CpG 岛超甲基化的沉默基因的方法，以及治疗和预防癌症和镰状细胞性贫血等疾病的方法，方法是施用一种调节甲基结合域（MBD）蛋白介导的转录抑制的制剂，从而增加基因转录以预防或治疗疾病。此外，还提供了本发明确定的有助于治疗和预防癌症和镰状细胞性贫血等疾病的化合物。
• Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such
  申请人：Southern Research Institute

  公开号：US10953017B2

  公开（公告）日：2021-03-23

  Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.

  本文描述了通过服用某些杂环化合物和芳香族化合物来增强记忆和/或学习能力并防止神经变性的方法。这些方法特别适用于治疗神经退行性疾病患者，如（但不限于）阿尔茨海默氏症、帕金森氏症、卢盖里氏症（ALS）或记忆或学习障碍。此外，还提供了一种基于神经元人体细胞的检测方法，利用荧光素酶报告物评估 NF-kB 基因的上调，从而筛选出在增强记忆或学习能力的方法中有用的化合物。
• Agents for Reversing Epigenetic Silencing of Genes
  申请人：Nelson William G.

  公开号：US20100093768A1

  公开（公告）日：2010-04-15

  The present invention provides methods for discovering agents that are effective in reversing epigenetic silencing by inhibiting the interaction of methyl-binding (MBD) proteins with methylated genomic DNA. Also provided are methods for reactivating silenced genes having CpG island hypermethylation along with methods for treatment and prevention of diseases, such as cancer and sickle cell anemia, by administering an agent that modulates methyl-binding domain (MBD) protein-mediated transcriptional repression, thereby increasing gene transcription to prevent or treat disease. Additionally, compounds identified by the present invention useful for treatment and prevention of diseases, such as cancer and sickle cell anemia, are provided.
• TREATMENT OF NEURODEGENERATIVE DISEASES, CAUSATION OF MEMORY ENHANCEMENT, AND ASSAY FOR SCREENING COMPOUNDS FOR SUCH
  申请人：Grimaldi Maurizio

  公开号：US20120245166A1

  公开（公告）日：2012-09-27

  Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.
• AGENTS FOR REVERSING EPIGENETIC SILENCING OF GENES
  申请人：The Johns Hopkins University

  公开号：US20150252438A1

  公开（公告）日：2015-09-10

  The present invention provides methods for discovering agents that are effective in reversing epigenetic silencing by inhibiting the interaction of methyl-binding (MBD) proteins with methylated genomic DNA. Also provided are methods for reactivating silenced genes having CpG island hypermethylation along with methods for treatment and prevention of diseases, such as cancer and sickle cell anemia, by administering an agent that modulates methyl-binding domain (MBD) protein-mediated transcriptional repression, thereby increasing gene transcription to prevent or treat disease. Additionally, compounds identified by the present invention useful for treatment and prevention of diseases, such as cancer and sickle cell anemia, are provided.