N-Piperidin-3-ylmethyl-propionamide | 886507-05-7

• 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-Piperidin-3-ylmethyl-propionamide
• 英文别名: N-(piperidin-3-ylmethyl)propanamide
• CAS: 886507-05-7
• 化学式: C₉H₁₈N₂O
• 分子量: 170.255
• InChiKey: ABUOKCYGDYMIBL-UHFFFAOYSA-N

物化性质

• 沸点：
  339.3±15.0 °C(Predicted)
• 密度：
  0.951±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  41.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-Piperidin-3-ylmethyl-propionamide 、 4-氟苯磺酰氯 在 三乙胺 作用下， 以 氯仿 为溶剂， 反应 12.0h， 以35%的产率得到N-[[1-(4-fluorophenyl)sulfonylpiperidin-3-yl]methyl]propanamide
  参考文献：
  名称：

  Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers

  摘要：

  A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2007.10.050
• 作为产物：
  描述：

  Tert-butyl 3-[(propanoylamino)methyl]piperidine-1-carboxylate 在 盐酸 作用下， 以 乙酸乙酯 为溶剂， 反应 12.0h， 以69%的产率得到N-Piperidin-3-ylmethyl-propionamide
  参考文献：
  名称：

  Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers

  摘要：

  A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2007.10.050

文献信息

• [EN] ANTIMICROBIAL COMPOUNDS<br/>[FR] COMPOSÉS ANTIMICROBIENS
  申请人：CURZA GLOBAL LLC

  公开号：WO2019013789A1

  公开（公告）日：2019-01-17

  Disclosed are compounds of formula I: or pharmaceutically acceptable salts thereof. Compounds of formula I are anti-microbials that inhibit, for instance, Mycobacterium tuberculosis (Mtb) H37Ra. Compounds of formula I also have anti-tubercular activity, exhibit limited cytotoxicity, and inhibit protein synthesis. Processes for making compounds of formula I are also disclosed, as well as methods of using compounds of formula I for the treatment of bacterial infections, particularly tuberculosis.

  公开的是I式化合物：或其药用可接受的盐。I式化合物是抗微生物的，例如抑制结核分枝杆菌（Mtb）H37Ra的。I式化合物还具有抗结核活性，表现出有限的细胞毒性，并且抑制蛋白质合成。公开了制备I式化合物的方法，以及使用I式化合物治疗细菌感染，特别是结核病的方法。
• [EN] ANTIMICROBIAL COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS ANTIMICROBIENS ET LEURS UTILISATIONS
  申请人：CURZA GLOBAL LLC

  公开号：WO2019013790A1

  公开（公告）日：2019-01-17

  Disclosed are compounds of formula I: or pharmaceutically acceptable salts thereof. Compounds of formula I are anti-microbials that inhibit, for instance, Mycobacterium tuberculosis (Mtb) H37Ra. Compounds of formula I also have anti-tubercular activity, exhibit limited cytotoxicity, and inhibit protein synthesis. Processes for making compounds of formula I are also disclosed, as well as methods of using compounds of formula I for the treatment of bacterial infections, particularly tuberculosis.

  本发明涉及公式I的化合物或其药学上可接受的盐。公式I的化合物是抗微生物的，例如抑制结核分枝杆菌（Mtb）H37Ra。公式I的化合物也具有抗结核活性，表现出有限的细胞毒性，并抑制蛋白质合成。本发明还揭示了制备公式I的化合物的方法，以及使用公式I的化合物治疗细菌感染，特别是结核病的方法。
• NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO
  申请人：DYCK Brian

  公开号：US20110166116A1

  公开（公告）日：2011-07-07

  New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R 1 , R 2 , R 3 , n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.

  本发明披露了一种新化合物，其在治疗患者的各种代谢相关疾病方面具有用途。本发明的化合物具有结构（I）：其中R1、R2、R3、n、p、q和Ar的定义如本文所述，包括立体异构体和药物可接受的盐。本发明还披露了包括本发明化合物的制药组合物，以及与在需要时使用该化合物的相关方法。
• US8293729B2
  申请人：——

  公开号：US8293729B2

  公开（公告）日：2012-10-23
• Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers
  作者：Elisabetta Martini、Carla Ghelardini、Silvia Dei、Luca Guandalini、Dina Manetti、Michele Melchiorre、Monica Norcini、Serena Scapecchi、Elisabetta Teodori、Maria Novella Romanelli

  DOI：10.1016/j.bmc.2007.10.050

  日期：2008.2.1

  A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity. (C) 2007 Elsevier Ltd. All rights reserved.