1-乙基吩恶噻10,10-二氧化物 | 134476-36-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 中文名称: 1-乙基吩恶噻10,10-二氧化物
• 英文名称: 1-Ethylphenoxathiin 10,10-dioxide
• 英文别名: 1-ethylphenoxathiin-10,10-dioxide；1-ethylphenoxathiine 10,10-dioxide
• CAS: 134476-36-1
• 化学式: C₁₄H₁₂O₃S
• 分子量: 260.313
• InChiKey: HQSRQKBSOOZLHH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  51.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-乙基吩恶噻10,10-二氧化物 在 二异丁基氢化铝 作用下， 以 甲苯 为溶剂， 反应 5.0h， 生成 1-ethylphenoxathiin
  参考文献：
  名称：

  Selective Inhibitors of Monoamine Oxidase (MAO). 5. 1-Substituted Phenoxathiin Inhibitors Containing No Nitrogen That Inhibit MAO A by Binding It to a Hydrophobic Site

  摘要：

  It is believed that a monoamine oxidase (MAO) inhibitor specific for MAO A, which is reversibly bound to this enzyme and displaceable:by tyramine, will be an antidepressant which will not cause a rise in blood pressure when tyramine-containing foods are ingested. Some linear tricyclic compounds with a larger and a smaller group forming the central ring and with a lipophilic group ortho to the larger group (here mostly the SO2 function of phenoxathiin 10, -10-dioxide) are reported to have the sought properties. Potency appears to require short length and relatively small cross section for the substituent. The 1-ethyl (13), 1-vinyl (22), 1-trifluoromethyl (27), and 1-iodo (76) phenoxathiin dioxides had the best profiles. Structure-activity relationships, syntheses, and a possible rationale for the selectivity of these compounds and related tricyclics are given. Compound 13 was selected for further development. A summary of pharmacological data for 13 is given.

  DOI：

  10.1021/jm970862j
• 作为产物：
  描述：

  (+)-1-(1-hydroxyethyl)phenoxathiin 10,10-dioxide 在 palladium hydroxide - carbon 、 氢气 作用下， 生成 1-乙基吩恶噻10,10-二氧化物
  参考文献：
  名称：

  一种选择性，可逆的竞争性单胺氧化酶A抑制剂，不含氮，酪胺引起的血压升高的增强作用可忽略不计。

  摘要：

  DOI：

  10.1021/jm00113a039

文献信息

• Pharmacologically active compound and use
  申请人：Burroughs Wellcome Co.

  公开号：US05420156A1

  公开（公告）日：1995-05-30

  1-Ethylphenoxathiin 10,10-dioxide (I) ##STR1## inhibits monoamine oxidase-A and is useful in the treatment of disorders such as depression.

  1-乙基苯氧硫啶10,10-二氧化物（I）抑制单胺氧化酶A，对治疗抑郁等疾病有用。
• Pharmacologically active compound., preparation and use
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP0419157A2

  公开（公告）日：1991-03-27

  1-Ethylphenoxathiin 10,10-dioxide (I) inhibits monoamine oxidase-A and is useful in the treatment of disorders such as depression.

  1-Ethylphenoxathiin 10,10-dioxide (I) 抑制单胺氧化酶-A，可用于治疗抑郁症等疾病。
• METHODS OF NOVEL THERAPEUTIC CANDIDATE IDENTIFICATION THROUGH GENE EXPRESSION ANALYSIS IN PULMONARY ARTERIAL HYPERTENSION
  申请人：Vascular Biosciences, Inc.

  公开号：EP2977468A2

  公开（公告）日：2016-01-27

  The present invention discloses multiple treatment regimens for vascular-related diseases and disorders. The present invention provides for methods of treating vascular-related disorders based on gene expression studies from samples collected from individuals having symptoms of vascular-related disorders. Additionally, methods are disclosed involving diagnostic techniques to focus treatment regimens. Finally, methods of treating vascular-related disorder involving targeting microRNAs are also disclosed.

  本发明公开了血管相关疾病和紊乱的多种治疗方案。 本发明提供了基于从具有血管相关疾病症状的个体采集的样本中进行的基因表达研究来治疗血管相关疾病的方法。 此外，本发明还公开了涉及诊断技术的方法，以确定治疗方案的重点。 最后，本发明还公开了以 microRNA 为靶标治疗血管相关疾病的方法。
• Cell lines for virus production and methods of use
  申请人：University of Georgia Research Foundation, Inc.

  公开号：US10137188B2

  公开（公告）日：2018-11-27

  Provided herein are engineered cell lines. In some embodiments, cells of an engineered cell line have altered expression of a gene and/or altered expression of an miRNA, wherein the altered expression results in increased or decreased production of a virus. The virus is a picornavirus, such as a poliovirus or Enterovirus 71. Also provided herein are methods for using the engineered cells to produce virus, and methods for treating a subject having or at risk of having a viral infection.

  本文提供的是工程细胞系。在某些实施方案中，工程细胞系的细胞具有基因表达的改变和/或 miRNA 表达的改变，其中表达的改变导致病毒产量的增加或减少。病毒是皮卡病毒，如脊髓灰质炎病毒或肠道病毒 71。本文还提供了使用工程细胞产生病毒的方法，以及治疗有病毒感染或有病毒感染风险的受试者的方法。
• Compositions and therapy for substance addiction
  申请人：——

  公开号：US20020019421A1

  公开（公告）日：2002-02-14

  Inhibitors of monoamine oxidase used in combination with an addictive substance, or a pharmacological derivative or analogue thereof, are useful for the treatment of substance addiction disorders. In particular, the invention discloses compositions, and methods of use thereof, comprising selegiline and nicotine for the treatment of cigarette smokers wishing to abstain. The compositions and methods of use thereof include oral, inhalant, parenteral and transdermal patch modes of therapy, whereby the subject benefits from the combined effects of a monoamine oxidase inhibitor in combination with an addictive substance, or derivative thereof.

  单胺氧化酶抑制剂与成瘾物质或其药理衍生物或类似物结合使用，可用于治疗物质成瘾症。特别是，本发明公开了包含西格列汀和尼古丁的组合物及其使用方法，用于治疗希望戒烟的吸烟者。本发明的组合物及其使用方法包括口服、吸入、肠外和透皮贴剂等治疗模式，受试者可从单胺氧化酶抑制剂与成瘾物质或其衍生物的联合作用中获益。