tert-butyl N-[1-[methoxy(methyl)amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamate | 178549-93-4

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: tert-butyl N-[1-[methoxy(methyl)amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamate
• CAS: 178549-93-4
• 化学式: C₂₀H₂₆N₂O₄
• 分子量: 358.437
• InChiKey: LDOUVARGJMVDMU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  26
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  67.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl N-[1-[methoxy(methyl)amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamate 、 (4-n-hexylphenyl)magnesium bromide 在 三氟乙酸 作用下， 以 2-甲基四氢呋喃 、 二氯甲烷 为溶剂， 反应 18.0h， 生成
  参考文献：
  名称：

  Small Molecule Suppression of Carbapenem Resistance in NDM-1 Producing Klebsiella pneumoniae

  摘要：

  The already considerable global public health threat of multidrug-resistant Gram-negative bacteria has become even more of a concern following the emergence of New Delhi metallo-beta-lactamase (NDM-1) producing strains of Klebsiella pneumoniae and other Gram-negative bacteria. As an alternative approach to the traditional development of new bactericidal entities, we have identified a 2-aminoimidazole-derived small molecule that acts as an antibiotic adjuvant and is able to suppress resistance of a NDM-1 producing strain of K. pneumoniae to imipenem and meropenem, in addition to suppressing resistance of other beta-lactam nonsusceptible K. pneumoniae strains. The small molecule is able to lower carbapenem minimum inhibitory concentrations by up to 16-fold, while exhibiting little bactericidal activity itself.

  DOI：

  10.1021/ml200290p
• 作为产物：
  描述：

  2-[(叔丁氧羰基)氨基]-3-萘-2-基丙酸 、 N-甲基-N-甲氧基胺盐酸盐 在 (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 16.0h， 以82%的产率得到tert-butyl N-[1-[methoxy(methyl)amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamate
  参考文献：
  名称：

  Small Molecule Suppression of Carbapenem Resistance in NDM-1 Producing Klebsiella pneumoniae

  摘要：

  The already considerable global public health threat of multidrug-resistant Gram-negative bacteria has become even more of a concern following the emergence of New Delhi metallo-beta-lactamase (NDM-1) producing strains of Klebsiella pneumoniae and other Gram-negative bacteria. As an alternative approach to the traditional development of new bactericidal entities, we have identified a 2-aminoimidazole-derived small molecule that acts as an antibiotic adjuvant and is able to suppress resistance of a NDM-1 producing strain of K. pneumoniae to imipenem and meropenem, in addition to suppressing resistance of other beta-lactam nonsusceptible K. pneumoniae strains. The small molecule is able to lower carbapenem minimum inhibitory concentrations by up to 16-fold, while exhibiting little bactericidal activity itself.

  DOI：

  10.1021/ml200290p

文献信息

• Melanocortin receptor ligands
  申请人：The Procter & Gamble Company

  公开号：US20030109556A1

  公开（公告）日：2003-06-12

  Disclosed are MC-3/MC-4 receptor ligands, the ligands having the following formula: 1 wherein A is a conformationally restricted ring system selected from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; wherein said rings comprises from 5 to 8 atoms; and W is a unit which preferable comprises D-1-fluorophenyalanine, Y comprises a heteroatom, and Z comprises an aromatic carbocyclic ring. Also disclosed are pharmaceutical compositions comprising the ligands of the invention as well as methods of treating diseases mediated through MC-3/MC-4 receptors.

  本发明涉及MC-3/MC-4受体配体，该配体具有以下公式：1其中A是从以下组中选择的构象限制性环系统：a)非芳香碳环；b)芳香碳环；c)非芳香杂环；d)芳香杂环；其中所述环包含5至8个原子；W是一个单元，它更喜欢包含D-1-氟苯丙氨酸，Y包含一个杂原子，Z包含一个芳香碳环。本发明还涉及包含该配体的制药组合物，以及通过MC-3/MC-4受体介导的疾病的治疗方法。
• MELANOCORTIN RECEPTOR LIGANDS
  申请人：THE PROCTER & GAMBLE COMPANY

  公开号：EP1390361A2

  公开（公告）日：2004-02-25
• EP1390361A4
  申请人：——

  公开号：EP1390361A4

  公开（公告）日：2005-10-05
• US6911447B2
  申请人：——

  公开号：US6911447B2

  公开（公告）日：2005-06-28
• US7087759B2
  申请人：——

  公开号：US7087759B2

  公开（公告）日：2006-08-08