3,5-dibromo-4'-trifluoromethyl salicylanilide | 53607-05-9

• 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: 3,5-dibromo-4'-trifluoromethyl salicylanilide
• 英文别名: 3,5-dibromo-2-hydroxy-N-[4-(trifluoromethyl)phenyl]benzamide
• CAS: 53607-05-9
• 化学式: C₁₄H₈Br₂F₃NO₂
• 分子量: 439.026
• InChiKey: FLYZSJGIJYEAFV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  22
• 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：
  49.3
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  对三氟甲基苯胺 、 3,5-二溴-2-羟基苯甲酸 在 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 生成 3,5-dibromo-4'-trifluoromethyl salicylanilide
  参考文献：
  名称：

  Identification and synthesis of low-molecular weight cholecystokinin B receptor (CCKBR) agonists as mediators of long-term synaptic potentiation

  摘要：

  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.

  DOI：

  10.1007/s00044-019-02292-x

文献信息

• ACTIVE DELIVERY SYSTEMS FORMULATIONS
  申请人：HOMOLA Andrew M.

  公开号：US20100040565A1

  公开（公告）日：2010-02-18

  The present invention relates to active delivery system formulations, and methods of making and using the same. Said formulations, when applied to a substrate surface, form a protective coating on the surface and permit constituent active agents to act on the surface and in the surrounding medium.

  本发明涉及活性传递系统配方，以及制备和使用这些配方的方法。当这些配方应用到基底表面时，在表面形成一层保护性涂层，并允许组分活性剂在表面和周围介质中起作用。
• Antibacterial antiplaque mouthwash composition
  申请人：Colgate-Palmolive Company

  公开号：EP0579383A1

  公开（公告）日：1994-01-19

  An oral composition mouthwash or liquid dentifrice containing an aqueous vehicle acceptable vehicle including an alcohol, a substantially water-insoluble noncationic antibacterial antiplaque agent, such as 2,4,4'-trichloro-2'-hydroxy-diphenyl ether (triclosan) wherein the antiplaque agent is entirely dissolved in the solvent and the weight ratio of water to alcohol is in excess of about 10:1.

  一种口腔组合物漱口水或液体牙膏，含有可接受的水性载体，包括酒精、基本不溶于水的非阳离子抗菌消泡剂，如 2,4,4'-三氯-2'-羟基二苯醚（三氯生），其中消泡剂完全溶解在溶剂中，水与酒精的重量比超过约 10:1。
• Oral composition containing salicylanilide antibacterial agent
  申请人：Colgate-Palmolive Company

  公开号：EP0628302A2

  公开（公告）日：1994-12-14

  An antiplaque oral composition such as a gel, paste or mouthrinse which is comprised of a vehicle having incorporated therein as the antiplaque agent an effective amount of an antibacterial salicylanilide compound and a surfactant mixture of an anionic surfactant, a polyoxyethylene/polyoxypropylene block copolymer and a taurate salt, the pH of the composition being adjusted to a pH of at least 8.0. An antibacterial-enhancing agent such as an anionic polymeric polycarboxylate which enhances the delivery of the salicylanilide compound to and retention on oral tissue surfaces is optionally incorporated in the composition to improve the efficacy of the salicylanilide compound.

  一种抗口腔污垢组合物，如凝胶、糊剂或漱口水，它由一种载体组成，载体中含有有效量的抗菌水杨酰苯胺化合物和一种阴离子表面活性剂、聚氧乙烯/聚氧丙烯嵌段共聚物和一种牛磺酸盐的表面活性剂混合物作为抗口腔污垢剂，组合物的 pH 值至少调节到 8.0。为提高水杨酰苯胺化合物的功效，可选择在组合物中加入抗菌增强剂，如阴离子聚合物聚羧酸盐，以增强水杨酰苯胺化合物向口腔组织表面的递送和在口腔组织表面的保留。
• Oral compositions
  申请人：Colgate-Palmolive Company

  公开号：EP0692246A1

  公开（公告）日：1996-01-17

  Oral compositions comprising the combination of an effective surface tension reducing amount of an amphoteric surfactant and an effective antimicrobial amount of a blend of phenolic agents and a substantially water insoluble noncationic antibacterial agent, such as Triclosan, is disclosed. These compositions are indicated in the management or control of dental plaque.

  本发明公开了由有效降低表面张力的两性表面活性剂和有效抗菌量的酚类制剂混合物以及基本不溶于水的非阳离子抗菌剂（如三氯生）组合而成的口服组合物。这些组合物适用于控制牙菌斑。
• Antimicrobial oral composition
  申请人：Colgate-Palmolive Company

  公开号：EP0696449A2

  公开（公告）日：1996-02-14

  A oral composition which inhibits plaque formation and reduces gingivitis and caries comprising a substantially water insoluble noncationic antimicrobial agent, such as triclosan and an acid reducing agent, such as xylitol. The composition is a dentifrice containing a siliceous polishing agent.

  一种可抑制牙菌斑形成、减少牙龈炎和龋齿的口腔组合物，包含一种基本不溶于水的非阳离子抗菌剂（如三氯生）和一种酸还原剂（如木糖醇）。该组合物是一种含有硅抛光剂的牙膏。