N-((2R,3R,4S,5R)-3,4-Dihydroxy-5-hydroxymethyl-piperidin-2-yl)-acetamide | 176246-06-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: N-((2R,3R,4S,5R)-3,4-Dihydroxy-5-hydroxymethyl-piperidin-2-yl)-acetamide
• 英文别名: (2r,3r,4s,5r)-2-Acetamido-3,4-Dihydroxy-5-Hydroxymethyl-Piperidine；N-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)piperidin-2-yl]acetamide
• CAS: 176246-06-3
• 化学式: C₈H₁₆N₂O₄
• 分子量: 204.226
• InChiKey: IWVRQJNSUOIUFV-VGRMVHKJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.1
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  102
• 氢给体数：
  5
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  siastatin B methyl ester 在 sodium tetrahydroborate 作用下， 以 乙醇 为溶剂， 反应 6.0h， 以90%的产率得到N-((2R,3R,4S,5R)-3,4-Dihydroxy-5-hydroxymethyl-piperidin-2-yl)-acetamide
  参考文献：
  名称：

  Synthesis and activity of 1-N-iminosugar inhibitors, siastatin B analogues for α-N-acetylgalactosaminidase and β-N-acetylglucosaminidase

  摘要：

  N-Acetylgalactosamine-based 1-N-iminosugars, new types of glycosidase inhibitor have been synthesized by modeling on siastatin B, isolated from a Streptomyces culture. The analogues of siastatin B were proved to be potent inhibitors for alpha-N-acetylgalactosaminidase and/or beta-N-acetylglucosaminidase.

  DOI：

  10.1016/0968-0896(95)00166-2

文献信息

• Method for Treating Alzheimer's Disease Using Pharmacological Chaperones To Increase The Activity of Gangliosidases
  申请人：Wustman Brandon

  公开号：US20120309788A1

  公开（公告）日：2012-12-06

  The present invention relates to a method for treating an individual having Alzheimer's Disease by using pharmacological chaperones to increase the activity of gangliosidase and/or sialidase enzymes involved in ganglioside catabolism.

  本发明涉及一种治疗患有阿尔茨海默病的个体的方法，该方法使用药理伴侣增加参与神经节苷脂降解的神经节苷脂酶和/或唾液酸酶酶活性。
• Method for Treating Cerebral Amyloid Angiopathy Using Pharmacological Chaperones to Increase the Activity of Gangliosidases
  申请人：Amicus Therapeutics, Inc.

  公开号：US20150374733A1

  公开（公告）日：2015-12-31

  The present invention relates to a method for treating an individual having Cerebral Amyloid Angiopathy by using pharmacological chaperones to increase the activity of gangliosidase and/or sialidase enzymes involved in ganglioside catabolism.

  本发明涉及一种治疗患有脑淀粉样血管病的个体的方法，通过使用药理伴侣增加参与神经节苷脂降解的神经节苷脂酶和/或唾液酸酶酶活性。
• METHOD FOR TREATING ALZHEIMER'S DISEASE USING PHARMACOLOGICAL CHAPERONES TO INCREASE THE ACTIVITY OF GANGLIOSIDASES
  申请人：Amicus Therapeutics, Inc.

  公开号：EP2957295B1

  公开（公告）日：2017-08-02
• Advanced drug development and manufacturing
  申请人：Birnbaum Eva R.

  公开号：US20080220441A1

  公开（公告）日：2008-09-11

  X-ray fluorescence (XRF) spectrometry has been used for detecting binding events and measuring binding selectivities between chemicals and receptors. XRF may also be used for estimating the therapeutic index of a chemical, for estimating the binding selectivity of a chemical versus chemical analogs, for measuring post-translational modifications of proteins, and for drug manufacturing.
• US9044437B2
  申请人：——

  公开号：US9044437B2

  公开（公告）日：2015-06-02