10-(α-diethylaminopropionyl)phenothiazine | 13012-66-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 英文名称: 10-(α-diethylaminopropionyl)phenothiazine
• 英文别名: 10-(alpha-diethylaminopropionyl)phenothiazine；ASTRA1397；As-1397；10-(N,N-diethyl-alanyl)-phenothiazine；10-(N,N-Diaethyl-alanyl)-phenothiazin；10-(2-(Diethylamino)propionyl)phenothiazine；2-(diethylamino)-1-phenothiazin-10-ylpropan-1-one
• CAS: 13012-66-3
• 化学式: C₁₉H₂₂N₂OS
• 分子量: 326.462
• InChiKey: QCEWCMMSOWEHFC-UHFFFAOYSA-N

物化性质

• 熔点：
  99.5-100.5 °C
• 沸点：
  506.2±39.0 °C(Predicted)
• 密度：
  1.174±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  48.8
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 海关编码：
  2934300000

反应信息

• 作为产物：
  描述：

  吩噻嗪 以 甲苯 为溶剂， 反应 8.0h， 生成 10-(α-diethylaminopropionyl)phenothiazine
  参考文献：
  名称：

  Novel Heterobivalent Tacrine Derivatives as Cholinesterase Inhibitors with Notable Selectivity Toward Butyrylcholinesterase

  摘要：

  Two series of novel heterobivalent tacrine derivatives were synthesized. A trimethoxy substituted benzene was linked to the tacrine moiety by a hydrazide-based linker. The compounds were evaluated as cholinesterase inhibitors, and trimethoxybenzoic acid derivatives with 11- or 12-atom spacers were the most potent inhibitors of human acetylcholinesterase. The inhibitors showed a surprising selectivity toward human butyrylcholinesterase, where several trimethoxyphenylpropionic acid derivatives had IC50 values less than 250 mu M.

  DOI：

  10.1021/jm060742o

文献信息

• Methods of Treating Disorders Associated with Protein Aggregation
  申请人：Pak Stephen C.

  公开号：US20130024953A1

  公开（公告）日：2013-01-24

  The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti-protein aggregate (“APA”) compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.

  本发明涉及与蛋白质聚集相关的临床疾病的治疗方法，包括向受试者施用来自以下组中选择的抗蛋白质聚集（“APA”）化合物的有效量：哌唑酮，氟哌利多（例如氟哌利多盐酸盐），他莫昔芬（例如他莫昔芬柠檬酸盐），紫杉醇，蝉蜕素，蝉酸及其盐和结构相关化合物。本发明至少部分基于以下发现：上述每种化合物均能促进Caenorhabditis elegans模型系统中聚集的ATZ蛋白的降解。根据本发明，使用这些APA化合物之一或多个进行治疗，可用于缓解AT缺陷以及其他由蛋白质聚集标记的疾病的症状和体征，包括但不限于阿尔茨海默病、帕金森病和亨廷顿病。
• Microparticles with multiple fluorescent signals and methods of using same
  申请人：——

  公开号：US20040087032A1

  公开（公告）日：2004-05-06

  This invention provides a novel fluorescent particle including a core or carrier particle having on its surface a plurality of smaller polymeric particles or nanoparticles, which are stained with different fluorescent dyes. When excited by a light source they are capable of giving off multiple fluorescent emissions simultaneously, which is useful for multiplexed analysis of a plurality of analytes in a sample. The coupled complex particles carrying on their surface fluorescent nanoparticles, methods of preparing such polymer particles, and various applications and methods of using such particles are claimed.

  本发明提供了一种新型荧光颗粒，包括一个核心或载体颗粒，其表面有多个较小的聚合物颗粒或纳米颗粒，这些颗粒被不同的荧光染料染色。当被光源激发时，它们能够同时发出多种荧光，这有助于对样品中的多种分析物进行多重分析。本发明提出了在其表面携带荧光纳米粒子的耦合复合粒子、制备这种聚合物粒子的方法以及使用这种粒子的各种应用和方法。
• MICROPARTICLES WITH MULTIPLE FLUORESCENT SIGNALS
  申请人：Luminex Corporation

  公开号：EP1049807B1

  公开（公告）日：2003-05-07
• MICROPARTICLES WITH MULTIPLE FLUORESCENT SIGNALS AND METHODS OF USING SAME
  申请人：Luminex Corporation

  公开号：EP1204869A1

  公开（公告）日：2002-05-15
• METHOD FOR ANALYZING A NUMBER OF SAMPLES FROM A VARIETY OF SOURCES FOR A SINGLE ANALYTE
  申请人：Luminex Corporation

  公开号：EP1204869B1

  公开（公告）日：2008-10-22