2-([Biphen-4-yloxy]ethyl)isoindoline-1,3-dione

• 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: 2-([Biphen-4-yloxy]ethyl)isoindoline-1,3-dione
• 英文别名: 2-[2-(4-phenylphenoxy)ethyl]isoindole-1,3-dione
• 化学式: C₂₂H₁₇NO₃
• 分子量: 343.382
• InChiKey: VBOHFFMFNFVNFS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-([Biphen-4-yloxy]ethyl)isoindoline-1,3-dione 在 一水合肼 作用下， 以 乙醇 为溶剂， 反应 4.0h， 生成 2-([1,1'-biphenyl]-4-yloxy)ethan-1-amine
  参考文献：
  名称：

  Identification of N-(2-Phenoxyethyl)imidazo[1,2-a]pyridine-3-carboxamides as New Antituberculosis Agents

  摘要：

  A series of inaidazo[1,2-a]pyridine carboxamides (IPAs) bearing an N-(2-phenoxyethyl) moiety was designed and synthesized as new antitubercular agents. Seven 2,6-dimethyl IPAs demonstrated excellent in vitro activity (MIC: 0.025-0.054 mu g/mL) against the drug susceptive H37Rv strain and two clinically isolated multidrug-resistant Mycobacterium tuberculosisstrains. Compound 10j displayed acceptable safety and pharmacokinetic properties, opening a new direction for further development. KEYWORDS: Antitubercular agents., MTB H37Rv, multidrug resistant-MTB,

  DOI：

  10.1021/acsmedchemlett.6b00330
• 作为产物：
  描述：

  N-羟乙基酞酰亚胺 、 对羟基联苯 在 三苯基膦 、 偶氮二甲酸二乙酯 作用下， 以 四氢呋喃 为溶剂， 生成 2-([Biphen-4-yloxy]ethyl)isoindoline-1,3-dione
  参考文献：
  名称：

  Identification of N-(2-Phenoxyethyl)imidazo[1,2-a]pyridine-3-carboxamides as New Antituberculosis Agents

  摘要：

  A series of inaidazo[1,2-a]pyridine carboxamides (IPAs) bearing an N-(2-phenoxyethyl) moiety was designed and synthesized as new antitubercular agents. Seven 2,6-dimethyl IPAs demonstrated excellent in vitro activity (MIC: 0.025-0.054 mu g/mL) against the drug susceptive H37Rv strain and two clinically isolated multidrug-resistant Mycobacterium tuberculosisstrains. Compound 10j displayed acceptable safety and pharmacokinetic properties, opening a new direction for further development. KEYWORDS: Antitubercular agents., MTB H37Rv, multidrug resistant-MTB,

  DOI：

  10.1021/acsmedchemlett.6b00330

文献信息

• Substituted heteroaryl- and phenylsulfamoyl compounds
  申请人：Hamanaka S. Ernest

  公开号：US20050288340A1

  公开（公告）日：2005-12-29

  The present invention is directed at substituted heteroaryl- and phenylsulfamoyl compounds, pharmaceutical compositions containing such compounds and the use of such compounds as peroxisome proliferator activator receptor (PPAR) agonists. PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans. The compounds are also useful for the treatment of negative energy balance (NEB) and associated diseases in ruminants.

  本发明涉及取代杂环芳基和苯基磺酰胺化合物，包含这些化合物的制药组合物和将这些化合物用作过氧化物酶增殖剂受体（PPAR）激动剂。PPARα激动剂，包含这些化合物的制药组合物，以及将这些化合物用于提高某些血浆脂质水平，包括高密度脂蛋白胆固醇和降低其他某些血浆脂质水平，如低密度脂蛋白胆固醇和甘油三酯，因此治疗由低高密度脂蛋白胆固醇水平和/或高低密度脂蛋白胆固醇和甘油三酯水平加重的疾病，例如动脉粥样硬化和心血管疾病，在哺乳动物中，包括人类。这些化合物还可用于治疗反能量平衡（NEB）和反刍动物相关疾病。
• Substituted Heteroaryl- and Phenylsulfamoyl Compounds
  申请人：Hamanaka S. Ernest

  公开号：US20060229363A1

  公开（公告）日：2006-10-12

  The present invention is directed at substituted heteroaryl and phenylsulfamoyl compounds, pharmaceutical compositions containing such compounds and the use of such compounds as peroxisome proliferator activator receptor (PPAR) agonists. PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides such as atherosclerosis and cardiovascular diseases, in mammals, including humans. The compounds are also useful for the treatment of negative energy balance (NEB) and associated diseases in ruminants.

  本发明涉及取代杂环芳基和苯基磺酰胺化合物、含有该类化合物的药物组合物及其作为过氧化物酶体增殖物激活受体（PPAR）激动剂的用途。该化合物可以作为PPARα激动剂，含有该类化合物的药物组合物可用于提高某些血浆脂质水平，包括高密度脂蛋白胆固醇，并降低其他某些血浆脂质水平，如低密度脂蛋白胆固醇和甘油三酯，从而治疗低高密度脂蛋白胆固醇水平和/或高低密度脂蛋白胆固醇和甘油三酯水平加剧的疾病，如动脉硬化和心血管疾病，在哺乳动物，包括人类中使用。该化合物还可用于治疗反能量平衡（NEB）和反刍动物相关疾病。
• Substituted alpha-aminosulphonyl-acetohydroxamic acids as therapeutic
  申请人：Pfizer Inc

  公开号：US06090852A1

  公开（公告）日：2000-07-18

  Compounds of formula (I): ##STR1## where the substituents are as defined herein, and salts thereof, are matrix metalloprotease inhibitors.

  式(I)的化合物：##STR1## 其中取代基的定义如本文所述，以及其盐，均为基质金属蛋白酶抑制剂。
• SUBSTITUTED HETEROARYL- AND PHENYLSULFAMOYL COMPOUNDS
  申请人：HAMANAKA S. ERNEST

  公开号：US20080090829A1

  公开（公告）日：2008-04-17

  The present invention is directed at substituted heteroaryl- and phenylsulfamoyl compounds, pharmaceutical compositions containing such compounds and the use of such compounds as peroxisome proliferator activator receptor (PPAR) agonists. PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans. The compounds are also useful for the treatment of negative energy balance (NEB) and associated diseases in ruminants.

  本发明涉及取代杂环芳基和苯基磺酰胺化合物，含有这种化合物的药物组合物以及将这种化合物用作过氧化物酶体增殖物激活受体（PPAR）激动剂。PPARα激动剂，含有这种化合物的药物组合物以及使用这种化合物升高某些血浆脂质水平，包括高密度脂蛋白胆固醇并降低其他某些血浆脂质水平，如低密度脂蛋白胆固醇和甘油三酯，并因此治疗低密度脂蛋白胆固醇和/或高甘油三酯水平加重的疾病，如动脉粥样硬化和心血管疾病，在哺乳动物中，包括人类。这些化合物还可用于治疗反能量平衡（NEB）和反刍动物相关疾病。