1-biphenyl-3-ylmaleimide | 840471-58-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-biphenyl-3-ylmaleimide
• 英文别名: 1-(biphenyl-3-yl)-1H-pyrrole-2,5-dione；1-(3-phenylphenyl)pyrrole-2,5-dione
• CAS: 840471-58-1
• 化学式: C₁₆H₁₁NO₂
• 分子量: 249.269
• InChiKey: QQAJYNGNBJIZPR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-biphenyl-3-ylmaleimide 、 Tert-butyl-(4-ethenyl-7-methoxy-2,2-dimethylchromen-8-yl)oxy-dimethylsilane 以 甲苯 为溶剂， 反应 24.0h， 生成
  参考文献：
  名称：

  Antidiabetic and Antiobesity Effects of Ampkinone (6f), a Novel Small Molecule Activator of AMP-Activated Protein Kinase

  摘要：

  Adenosine 5'-monophosphate (AMP) activated protein kinase (AMPK) has emerged as an attractive target molecule for the treatment of metabolic disorders, including obesity and type 2 diabetes. In this study, we identified a novel small molecule, ampkinone (6f), as an indirect AMPK activator, which was derived from the small molecule library constructed by diversity-oriented synthesis. Ampkinone stimulated the phosphorylation of AMPK via the indirect activation of AMPK in various cell lines. Ampkinone-mediated activation of AMPK required the activity of LKB1 and resulted in increased glucose uptake in muscle cells. In addition, ampkinone-treated DIO mice significantly reduced total body weight and overall fat mass. Histological examination and measurement of lipid parameters showed that ampkinone effectively improved metabolic abnormalities in the DIO mice model. Our results demonstrate that ampkinone, a small molecule with a privileged benzopyran substructure, has a potential as a new class of therapeutic agent for antidiabetic and antiobesity treatment via the indirect stimulation of AMPK.

  DOI：

  10.1021/jm100565d
• 作为产物：
  描述：

  (Z)-3-(Biphenyl-3-ylcarbamoyl)-acrylic acid 在 sodium acetate 、 乙酸酐 作用下， 反应 0.5h， 生成 1-biphenyl-3-ylmaleimide
  参考文献：
  名称：

  N-取代的马来酰亚胺衍生物作为选择性甘油单酯脂肪酶抑制剂的合成及体外评价

  摘要：

  内源性大麻素2-花生四烯酸甘油酯（2-AG）在许多生理过程中起着重要作用，其作用通过甘油单酯脂肪酶（MGL）催化的酶促水解迅速终止。调节其内源水平可以提供治疗机会；然而，到目前为止，几乎没有描述选择性的MGL抑制剂。在这里，我们描述了N-取代的马来酰亚胺的合成及其对重组人脂肪酸酰胺水解酶（FAAH）和纯化人MGL的药理评价。先前已经描述了一些N-芳基马来酰亚胺（萨里奥（SM）；萨洛（OM）；Nevalainen，T .；Poso，A。莱蒂宁（JT）；贾文恩（T. Jarvinen）Niemi，R.大鼠小脑膜中2-花生四烯酸甘油水解酶中巯基敏感位点的表征。化学 生物学 2005年，12，649-656），为MGL抑制剂，以及沿着这些线路，我们提出一组新的马来酰亚胺衍生物的那显示出低微摩尔的IC 50和朝向MGL VS FAAH高选择性。然后，研究了结构活性关系，例如，1-biphenyl-4

  DOI：

  10.1021/jm900461w

文献信息

• [EN] ASPARTATES USEFUL AS COMPONENTS IN COATING COMPOSITIONS AND THEIR PREPARATION<br/>[FR] ASPARTATES UTILISES COMME CONSTITUANTS DANS DES COMPOSITIONS DE REVETEMENT, ET LEUR PREPARATION
  申请人：BAYER MATERIALSCIENCE LLC

  公开号：WO2005073188A1

  公开（公告）日：2005-08-11

  The present invention relates to novel aspartates, their method of production and the use of these aspartates as reactive components for polyisocyanates in two-component polyurethane coating compositions and for preparing polyurethane prepolymers. The aspartates are prepared by first reacting a di- or polyamine with an unsaturated ester and then reacting the resultant product with a maleimide.

  本发明涉及新颖的天冬氨酸、其制备方法以及将这些天冬氨酸作为双组分聚氨酯涂料组成部分的聚异氰酸酯反应组分和制备聚氨酯预聚体。这些天冬氨酸是通过首先将二元或多元胺与不饱和酯反应，然后将产物与马来酰亚胺反应制备而成。
• PROCESS FOR PREPARING ASPARTATES
  申请人：Danielmeier Karsten

  公开号：US20050159560A1

  公开（公告）日：2005-07-21

  The present invention relates to novel aspartates, their method of production and the use of these aspartates as reactive components for polyisocyanates in two-component polyurethane coating compositions and for preparing polyurethane prepolymers. The aspartates are prepared by first reacting a di- or polyamine with an unsaturated ester and then reacting the resultant product with a maleimide.

  本发明涉及新型天冬氨酸盐、其生产方法以及将这些天冬氨酸盐用作双组分聚氨酯 涂料组合物中多异氰酸酯的反应组分和制备聚氨酯预聚物。天冬氨酸盐的制备方法是首先使二元胺或多元胺与不饱和酯反应，然后使生成物与马来酰亚胺反应。
• Polyaspartimides
  申请人：Danielmeier Karsten

  公开号：US20060106194A1

  公开（公告）日：2006-05-18

  The present invention relates to novel polyaspartimides, their method of production and the use of these polyaspartimides as reactive components for polyisocyanates in two-component polyurethane coating compositions. The polyaspartimides are prepared by reacting a polyether amine with a maleimide.

  本发明涉及新型聚天冬氨酰亚胺、其生产方法以及将这些聚天冬氨酰亚胺用作双组分聚氨酯涂料组合物中聚异氰酸酯的反应组分。聚天冬酰亚胺是通过聚醚胺与马来酰亚胺反应制备的。
• Polyaspartimides useful as reactive components for polyisocyanates in two-component polyurethane coating compositions
  申请人：Bayer MaterialScience AG

  公开号：EP1666461B1

  公开（公告）日：2009-06-24
• ASPARTATES USEFUL AS COMPONENTS IN COATING COMPOSITIONS AND THEIR PREPARATION
  申请人：Bayer MaterialScience LLC

  公开号：EP1708995B1

  公开（公告）日：2013-02-27