N-(1,3-噻唑-2-基)丙烯酰胺 | 117158-04-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: N-(1,3-噻唑-2-基)丙烯酰胺
• 英文名称: N-(thiazol-2-yl)acrylamide
• 英文别名: 2-Acrylamidothiazole；N-(1,3-thiazol-2-yl)prop-2-enamide
• CAS: 117158-04-0
• 化学式: C₆H₆N₂OS
• 分子量: 154.192
• InChiKey: GJQQHYNZZYZIKE-UHFFFAOYSA-N

物化性质

• 密度：
  1.319±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  70.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-methyl-C-(diethoxyphosphoryl)nitrone 、 N-(1,3-噻唑-2-基)丙烯酰胺 以 甲苯 为溶剂， 反应 24.0h， 以40%的产率得到diethyl trans-5-(thiazol-2-ylcarbamoyl)-2-methylisoxazolidin-3-yl-3-phosphonate
  参考文献：
  名称：

  Novel 5-Arylcarbamoyl-2-methylisoxazolidin-3-yl-3-phosphonates as Nucleotide Analogues

  摘要：

  A series of 5-substituted 3-phosphonylated isoxazolidines have been obtained via cycloaddition of N-methyl-C-(diethoxyphosphoryl)nitrone with N-heteroaromatic acrylamides. Good trans/cis diastereoselectivities (d.e. 58-76%) of isomeric (3-diethoxyphosphoryl)isoxazolidines were observed. cis- and trans-Isoxazolidine phosphonates were evaluated for their antiviral activity against a broad range of DNA and RNA viruses but were found inactive. Their cytostatic activity toward L1210, CEM, and HeLa cells was also established, and compounds cis-12r and trans-11r having a 2,2-difluorobenzo[d][1,3]dioxole moiety slightly inhibited proliferation of HeLa cells at IC50 values of 186 and 179 μM, respectively.

  DOI：

  10.1080/15257770.2014.909046
• 作为产物：
  描述：

  2-氨基噻唑 、 丙烯酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 3.0h， 以80%的产率得到N-(1,3-噻唑-2-基)丙烯酰胺
  参考文献：
  名称：

  含3-氧代-N-烯丙基-1,2-苯并异噻唑-3(2H)-甲酰胺单体的丙烯酸酯共聚物作为海洋防污涂料的合成及生物活性

  摘要：

  通过甲基丙烯酸甲酯（MMA）与丁基丙烯酸酯共聚，合成了一种含有 3-氧代-N-烯丙基-1,2-苯并异噻唑-2（3 H ）-甲酰胺单体和杂环单体的接枝丙烯酸酯共聚物树脂。丙烯酸酯（BA）与功能单体。单体和共聚物的结构通过红外（IR）和1 H 核磁共振（NMR）光谱进行验证。测量了共聚物对藻类、细菌和藤壶幼虫的抑制活性，并研究了其对海洋大型生物的防污效力。结果表明，接枝树脂对三种海洋藻类（等鞭金藻、微绿绿藻和蛋白核小球藻）和三种细菌（解珊瑚弧菌、金黄色葡萄球菌和副溶血弧菌）的生长具有显着的抑制作用。目标共聚物还表现出对藤壶幼虫存活的优异抑制作用。此外，防污剂的释放速率和海洋现场测试结果表明，接枝共聚物对海洋大型污垢生物的附着具有出色的防污效力。

  DOI：

  10.1002/open.202000273

文献信息

• [EN] FTO INHIBITORS<br/>[FR] INHIBITEURS DE FTO
  申请人：NAT INST OF BIOLOGICAL SCIENCES BEIJING

  公开号：WO2016206573A1

  公开（公告）日：2016-12-29

  The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

  这项发明提供了抑制FTO（脂肪质量和肥胖）的化合物，包括药用可接受的盐、氢化物和立体异构体。这些化合物用于制备药物组合物，以及制备和使用的方法，包括使用有效量的化合物或组合物治疗有需要的人，特别是肥胖症，并检测人的健康或状况的改善。
• Vesicular monoamine transporter gene therapy in parkinson's disease
  申请人：——

  公开号：US20030143702A1

  公开（公告）日：2003-07-31

  The present invention provides methods and compositions for the therapeutic intervention of Parkinson's disease. More particularly, methods of making and sequestering dopamine are disclosed. Additionally, methods of genetically modifying donor cells by gene transfer for grafting into the central nervous system to treat defective, diseased or damaged cells are disclosed. Methods and compositions for carrying out such gene transfer and grafting are described.

  本发明提供了治疗干预帕金森病的方法和组合物。更具体地说，本发明公开了制造和封存多巴胺的方法。此外，本发明还公开了通过基因转移对供体细胞进行基因修饰的方法，以便将其移植到中枢神经系统中治疗有缺陷、患病或受损的细胞。还描述了进行这种基因转移和移植的方法和组合物。
• FTO INHIBITORS
  申请人：National Institute Of Biological Sciences, Beijing

  公开号：EP3303283A1

  公开（公告）日：2018-04-11
• Vesicular monoamine transporter gene therapy in Parkinson's disease
  申请人：Kang Un Jung

  公开号：US20090036393A1

  公开（公告）日：2009-02-05

  The present invention provides methods and compositions for the therapeutic intervention of Parkinson's disease. More particularly, methods of making and sequestering dopamine are disclosed. Additionally, methods of genetically modifying donor cells by gene transfer for grafting into the central nervous system to treat defective, diseased or damaged cells are disclosed. Methods and compositions for carrying out such gene transfer and grafting are described.
• Inhibitors of heat shock factors and uses thereof
  申请人：Vilaboa Nuria

  公开号：US20210221778A1

  公开（公告）日：2021-07-22

  The present disclosure relates to a class of mammalian heat shock factor (HSF) inhibitors, to pharmaceutical compositions comprising these inhibitors as well as to methods for using the inhibitors. The inhibitors inhibit stress-induced expression from heat shock gene promoters. Furthermore, the inhibitors are cytotoxic to a variety of human cancer cells types.