5-amino-2-hydroxy-N-(4-trifluoromethylphenyl)benzamide | 1285539-51-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-amino-2-hydroxy-N-(4-trifluoromethylphenyl)benzamide
• 英文别名: 5-amino-2-hydroxy-N-[4-(trifluoromethyl)phenyl]benzamide
• CAS: 1285539-51-6
• 化学式: C₁₄H₁₁F₃N₂O₂
• 分子量: 296.249
• InChiKey: QFPVRIQHUCEYIB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  75.4
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-hydroxy-5-nitro-N-[4-(trifluoromethyl)phenyl]benzamide 在 palladium on activated charcoal 、 氢气 作用下， 以 乙酸乙酯 为溶剂， 反应 1.0h， 以33%的产率得到5-amino-2-hydroxy-N-(4-trifluoromethylphenyl)benzamide
  参考文献：
  名称：

  作为镇痛药的新型环加氧酶-1抑制剂的设计与合成：5-氨基-2-乙氧基-N-（取代苯基）苯甲酰胺

  摘要：

  我们以前发现，COX-1抑制剂N-（4-氨基苯基）-4-三氟甲基苯甲酰胺（TFAP）具有镇痛作用，而不会引起胃部损害。不幸的是，TFAP引起尿液呈紫红色，其镇痛作用不如消炎痛。在这里，我们描述我们的研究，重点是根据TFAP和帕拉沙米（另一种已知的COX-1抑制镇痛药）的结构设计的4和5-氨基-2-烷氧基-N-苯基苯甲酰胺支架的开发。5-氨基-2-乙氧基N-（2-或3-取代苯基）苯甲酰胺衍生物在鼠乙酸诱导的扭体试验中显示出镇痛活性。在这些化合物中，5-氨基-2-乙氧基N-（2-甲氧基苯基）苯甲酰胺（9 v）具有有效的COX-1抑制和镇痛活性，类似于消炎痛。此外，5-氨基-2-乙氧基N-（3-三氟甲基苯基）苯甲酰胺（9 g）比消炎痛或9 v具有更强的镇痛作用，尽管对COX-1具有抑制作用，但不会引起明显的胃部损害或尿液着色。活性弱于消炎痛或9 v。因此，9 g和9 v似乎是有希望用作止痛药的候

  DOI：

  10.1002/cmdc.201000462

文献信息

• N-4-三氟甲基苯基水杨酰胺衍生物的制备方 法和应用
  申请人：中国科学院广州生物医药与健康研究院

  公开号：CN104873522B

  公开（公告）日：2019-06-04

  本发明公开了一种通式（Ⅰ）为N‑4‑三氟甲基苯基水杨酰胺衍生物的制备方法和应用。N‑4‑三氟甲基苯基水杨酰胺衍生物或药学上可接受的盐的制备方法具有反应原料易得，操作简便等优点，适合工业化生产。所述N‑4‑三氟甲基苯基水杨酰胺衍生物对结核菌标准株H37Rv和临床耐药结核菌的生长具有较强的抑制作用，可用于制备抗结核病的药物中，最低抑菌浓度可以达到5μg/mL。
• Identification and synthesis of low-molecular weight cholecystokinin B receptor (CCKBR) agonists as mediators of long-term synaptic potentiation
  作者：Yanmei Zhang、Yican Wang、Yiping Guo、Jinxi Liao、Zhengchao Tu、Yongzhi Lu、Ke Ding、Micky D. Tortorella、Jufang He

  DOI：10.1007/s00044-019-02292-x

  日期：2019.3

  Recently, He et al. reported that CCKB receptors located in the neocortex of the brain when bound to their bound natural ligand, CCK peptides, enhance memory, bringing up the possibility that agonists targeting the CCKB receptor may act as therapeutic agents in diseases in which memory loss is marked as observed in dementia and Alzheimer's. In this report, we describe the synthesis of novel low-molecular weight benzoamine CCKB receptor agonists. The compounds made in this series were determined to be mostly partial agonists, although some antagonists were identified, as well, capable of triggering calcium release in a cell line that overexpresses the CCKB receptor. Compound 35 demonstrated an EC50 of 0.15 mu M in the cell-based assay, but more importantly, several of the compounds, including 35, demonstrated a physiological effect, inducing long-term potentiation in rat brains comparable to the CCK-8 peptide albeit at much higher concentrations. Based on these findings, benzoamines may be the basis for a new series of CCKB receptor agonists in drug-discovery efforts that seek to develop therapeutics to prevent memory loss.
• PROCESS FOR DYEING IN THE PRESENCE OF OXIDATION BASES COMPRISING AT LEAST ONE SULFONIC, SULFONAMIDE, SULFONE, AMID OR ACID GROUP AND A METAL CATALYST, DEVICE AND READY-TO-USE COMPOSITION
  申请人：L'OREAL

  公开号：US20160143826A1

  公开（公告）日：2016-05-26

  The present invention relates to a process for dyeing human keratin fibres, in which use is made of one or more metal catalysts and a composition (A) comprising: (a) at least 10% by weight of one or more fatty substances, (b) one or more oxidation bases of formula (I) or (II), the addition salts thereof, solvates thereof and mixtures thereof: Formula (I), Formula (II) (c) one or more chemical oxidizing agents other than atmospheric oxygen. The invention also relates to a multi-compartment device and to a composition comprising all of the above-mentioned ingredients.
• US9872822B2
  申请人：——

  公开号：US9872822B2

  公开（公告）日：2018-01-23