2-BuMP | 143346-99-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-BuMP
• 英文别名: N-(2-butyl)-N-methylpropargylamine；sec-Butyl-methyl-prop-2-ynyl-amine; oxalic acid with HCl；N-methyl-N-prop-2-ynylbutan-2-amine
• CAS: 143346-99-0
• 化学式: C₈H₁₅N
• 分子量: 125.214
• InChiKey: CJRQAPHWCGEATR-UHFFFAOYSA-N

物化性质

• 沸点：
  153.5±13.0 °C(Predicted)
• 密度：
  0.823±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  9
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  N-甲基炔丙基胺 、 2-溴丁烷 在 sodium carbonate 作用下， 以 乙醇 为溶剂， 反应 72.0h， 生成 2-BuMP
  参考文献：
  名称：

  Aliphatic propargylamines: potent, selective, irreversible monoamine oxidase B inhibitors

  摘要：

  A series of aliphatic propargylamine derivatives has been synthesized. Some of them possess highly potent, irreversible, selective, inhibitory activity toward monoamine oxidase B (MAO-B). The potency of the inhibitors is related to chain length and substitution of a hydrogen on the terminal carbon of the aliphatic chain. MAO inhibitory activity as assessed in vitro increased as the aliphatic carbon chain length increased. Substitution of a hydrogen by hydroxyl, carboxyl, or carbethoxyl groups at the aliphatic chain terminal or replacement of the methyl group on the nitrogen atom by an ethyl group considerably reduced the inhibitory activity. Stereospecific effects were observed with the R-(-)-enantiomer being 20-fold more active than the S-(+)-enantiomer. Inhibitors with relatively short carbon chain lengths (i.e. four to six carbons) were found to be more potent than those with longer chains in inhibiting brain MAO-B activity in vivo especially after oral administration. Chronic administration of low doses of the aliphatic propargylamines caused a slight cumulative inhibition of MAO-A activity in the mouse brain. These MAO-B inhibitors appear to be nontoxic, and they do not possess an amphetamine-like moiety in their structure as is the case for deprenyl. We expect that these aliphatic propargylamines may be useful in the treatment in certain neuropsychiatric disorders.

  DOI：

  10.1021/jm00098a017

文献信息

• [EN] LACTONE INTERMEDIATES OF NICOTINAMIDE RIBOSIDE AND NICOTINATE RIBOSIDE<br/>[FR] INTERMÉDIAIRES DE LACTONE DE NICOTINAMIDE RIBOSIDE ET DE NICOTINATE RIBOSIDE
  申请人：UNIV BELFAST

  公开号：WO2018033639A1

  公开（公告）日：2018-02-22

  The present invention is directed to lactones of the following structural formula for use as precursors of NAD, and their use as nutritional supplements.

  本发明涉及以下结构式的内酯，用作NAD的前体，并且它们的用途作为营养补充剂。
• [EN] PREPARATION AND USE OF CRYSTALLINE BETA-D-NICOTINAMIDE RIBOSIDE<br/>[FR] PRÉPARATION ET UTILISATION DE BÊTA-D-NICOTINAMIDE RIBOSIDE CRISTALLIN
  申请人：GLAXOSMITHKLINE IP NO 2 LTD

  公开号：WO2015186068A1

  公开（公告）日：2015-12-10

  Provided herein are crystalline beta-D-nicotinamide riboside chloride compositions and methods of preparation and use thereof. Also provided are related pharmaceutical compositions and methods of use thereof. The crystalline beta-D-nicotinamide riboside chloride compositions may be used to treat a disease or disorder that would benefit from increased NAD levels including a mitochondrial disease or disorder, insulin resistance, a metabolic syndrome, diabetes, obesity, or for increasing insulin sensitivity in a subject.

  本文提供晶体质的β-D-烟酰胺核苷酸氯化物组合物的制备和使用方法。还提供相关的药物组合物及其使用方法。晶体质的β-D-烟酰胺核苷酸氯化物组合物可用于治疗需要提高NAD水平的疾病或疾病，包括线粒体疾病或疾病，胰岛素抵抗，代谢综合征，糖尿病，肥胖症或用于增加受试者胰岛素敏感性。
• AMINOQUINOLINE DERIVATIVES AND USES THEREOF
  申请人：THE MCLEAN HOSPITAL CORPORATION

  公开号：US20150023930A1

  公开（公告）日：2015-01-22

  Described herein are aminoquinoline and aminoacridine based hybrids, pharmaceutical compositions and medicaments that include such aminoquinoline and aminoacridine based hybrids, and methods of using such compounds for diagnosing and/or treating infections, neurodegerative diseases or disorders, inflammation, inflammation associated diseases and disorders, and/or diseases or disorders that are treatable with dopamine agonists such as the restless leg syndrome.

  本文描述了基于氨基喹啉和氨基蒽醌的混合物，包括含有这种基于氨基喹啉和氨基蒽醌的混合物的制药组合物和药物，以及使用这种化合物诊断和/或治疗感染、神经退行性疾病或障碍、炎症、与炎症相关的疾病和障碍以及可用多巴胺激动剂治疗的疾病或障碍（如不宁腿综合征）的方法。
• METHODS OF ADMINSTERING AN AMPA RECEPTOR ANTAGONIST TO TREAT DYSKINESIAS ASSOCIATED WITH DOPAMINE AGONIST THERAPY
  申请人：——

  公开号：US20010034345A1

  公开（公告）日：2001-10-25

  The invention relates to a method of treating dyskinesias associated with dopamine agonist therapy in a mammal which comprises administering to said mammal an effective amount of an antagonist of the AMPA receptor. Dopamine agonist therapy, as referred to in the present invention, is generally used in the treatment of a central nervous system disorder such as Parkinson's disease.

  本发明涉及一种治疗哺乳动物多巴胺激动剂治疗相关运动障碍的方法，其包括向该哺乳动物施用有效量的AMPA受体拮抗剂。本发明所指的多巴胺激动剂治疗通常用于治疗中枢神经系统疾病，如帕金森病。
• Modulators of CDC2-like kinases (CLKS) and methods of use thereof
  申请人：Milne Jill

  公开号：US20070248590A1

  公开（公告）日：2007-10-25

  Provided herein are methods for using Cdc2-like kinase (Clk) modulators for treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, ocular disorders, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a Clk modulating compound in combination with another therapeutic agent.

  本文提供了使用Cdc2-like kinase (Clk)调节剂治疗和/或预防各种疾病和障碍的方法，包括与衰老或压力有关的疾病或障碍、糖尿病、肥胖症、神经退行性疾病、心血管疾病、血液凝结障碍、炎症、癌症、眼部疾病和/或潮红，以及需要增加线粒体活动的疾病或障碍。此外，提供了包含Clk调节化合物与另一种治疗剂联合使用的组合物。