1-(2-Aminoacetamido)-2-methylpropan | 590423-20-4

• 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: 1-(2-Aminoacetamido)-2-methylpropan
• 英文别名: 2-amino-N-isobutyl-acetamide；2-amino-N-isobutylethanamide；isobutylglycinamide；2-amino-N-isobutylacetamide；2-amino-N-(2-methylpropyl)acetamide
• CAS: 590423-20-4
• 化学式: C₆H₁₄N₂O
• mdl: MFCD09724195
• 分子量: 130.19
• InChiKey: RRSSLJCGIBNHIW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  9
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.833
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(2-Aminoacetamido)-2-methylpropan 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 potassium phosphate 、 四(三苯基膦)钯 、 potassium acetate 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 作用下， 以 DMP 、 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  新型2-（6-氨基甲基芳基-2-芳基-4-氧代-喹唑啉-3（4 H）-基）乙酰胺加压素V 1b受体拮抗剂的合成与合成孔径雷达研究

  摘要：

  合成和结构-活性关系（SAR）的一系列新的加压素V 1b拮抗剂。已经鉴定出2-（6-氨基甲基芳基-2-芳基-4-氧代-喹唑啉-3（4H）-基）乙酰胺对V 1b受体具有低纳摩尔摩尔亲和力，并且对相关受体V 1a，V具有良好的选择性2和OT。优化的化合物16在HPA功能障碍的机械模型中显示出良好的药代动力学特征和活性。

  DOI：

  10.1016/j.bmcl.2011.04.022
• 作为产物：
  描述：

  Benzyloxycarbonylglycin-isobutylamid 在 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 为溶剂， 20.0 ℃ 、101.33 kPa 条件下， 反应 3.0h， 以94%的产率得到1-(2-Aminoacetamido)-2-methylpropan
  参考文献：
  名称：

  Synthesis, physical–chemical characterisation and biological evaluation of novel 2-amido-3-hydroxypyridin-4(1H)-ones: Iron chelators with the potential for treating Alzheimer’s disease

  摘要：

  A novel class of 2-amido-3-hydroxypyridin-4-one iron chelators is described. These compounds have been designed to behave as suitable molecular probes which will improve our knowledge of the role of iron in neurodegenerative conditions. Neurodegenerative disorders, such as Alzheimer's disease (AD) and Parkinson disease (PD), can be considered as diverse pathological conditions sharing critical metabolic processes such as protein aggregation and oxidative stress. Interestingly, both these metabolic alterations seem to be associated with the involvement of metal ions, including iron. Iron chelation is therefore a potential therapeutic approach. The physico-chemical (pK(a) pFe(3+) and log P) and biological properties (inhibition of iron-containing enzymes) of these chelators have been investigated in order to obtain a suitable profile for the treatment of neurodegenerative conditions. Studies with neuronal cell cultures confirm that the new iron chelators are neuroprotective against beta-amyloid-induced toxicity. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2010.12.007

文献信息

• [EN] NEW USE OF PYRIMIDINE - OR TRIAZINE- 2-CARBONITILES FOR TREATING DISEASES ASSOCIATED WITH CYSTEINE PROTEASE ACTIVITY AND NOVEL PYRIMIDINE-2-CARBONITILE DERIVATIVES<br/>[FR] NOUVELLE UTILISATION DE PYRIMIDINE - OU TRIAZINE- 2-CARBONITILES DESTINES AU TRAITEMENT DE MALADIES LIEES A L'ACTIVITE DE PROTEASE A CYSTEINE ET NOUVEAUX DERIVES DE PYRIMIDINE-2-CARBONITILE
  申请人：ASTRAZENECA AB

  公开号：WO2004000819A1

  公开（公告）日：2003-12-31

  The present invention therefore provides use of a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition, this invention also discloses processes for the preparation of such inhibitors.

  因此，本发明提供了一种使用化合物(I)和组合物治疗与半胱氨酸蛋白酶活性相关疾病的方法。这些化合物是半胱氨酸蛋白酶S、K、F、L和B的可逆抑制剂。特别感兴趣的是与S半胱氨酸蛋白酶相关的疾病。此外，本发明还揭示了制备这些抑制剂的方法。
• COMPOUNDS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASE
  申请人：SHY Therapeutics LLC

  公开号：US20170174699A1

  公开（公告）日：2017-06-22

  Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.

  本文提供了抑制MAPK磷酸化的化合物，因此可用于治疗癌症和炎症性疾病的组合物和方法。
• Methods for treating anthrax and inhibiting lethal factor
  申请人：Hermes Jeffery D.

  公开号：US20100003276A1

  公开（公告）日：2010-01-07

  This invention relates to a method of inhibiting lethal factor (LF) or for treating anthrax and other conditions related to anthrax infection comprising co-administration of an effective amount of an LF inhibitor and a vaccine to a patient in need of such treatment. Such co-administration unexpectedly provides an effective immune response.

  这项发明涉及一种抑制致死因子（LF）或用于治疗炭疽病和与炭疽感染相关的其他疾病的方法，包括向需要此类治疗的患者联合给予有效剂量的LF抑制剂和疫苗。这种联合给药意外地提供了有效的免疫反应。
• 2-(4-Oxo-4H-Quinazolin-3-Yl) Acetamides and Their Use as Vasopressin V3 Antagonists
  申请人：Letourneau Jeffrey

  公开号：US20080214553A1

  公开（公告）日：2008-09-04

  The present invention relates to 2-(4-oxo4H-quinazolin-3-yl)acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.

  本发明涉及公式（I）的2-（4-氧代4H-喹唑啉-3-基）乙酰胺衍生物，以及它们作为利尿激素V3拮抗剂的用途，特别是用于治疗抑郁症。
• ESTER PRO-DRUGS OF [3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL] METHANOL FOR TREATING RETINAL DISEASES
  申请人：Dibas Mohammed I.

  公开号：US20120149746A1

  公开（公告）日：2012-06-14

  The present invention relates to method of treating retinal diseases in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

  本发明涉及一种治疗视网膜疾病的方法，适用于需要此类治疗的受试者，包括给予含有[3-(1-(1H-咪唑-4-基)乙基)-2-甲基苯基]甲醇酯前药的治疗有效剂量组成物，制备它们的方法，含有它们的制药组合物以及它们作为药物的用途。