1-(4-acetylphenyl)-3-(4-bromophenyloxy)pyrrolidine-2,5-dione | 1415914-22-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-(4-acetylphenyl)-3-(4-bromophenyloxy)pyrrolidine-2,5-dione
• 英文别名: 1-(4-Acetylphenyl)-3-(4-bromophenoxy) pyrrolidine-2,5-dione；1-(4-acetylphenyl)-3-(4-bromophenoxy)pyrrolidine-2,5-dione
• CAS: 1415914-22-5
• 化学式: C₁₈H₁₄BrNO₄
• 分子量: 388.217
• InChiKey: PFGMNECTQWLUHH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  63.7
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-氨基苯乙酮 在 三乙烯二胺 作用下， 以 乙醚 、 水 为溶剂， 反应 1.5h， 生成 1-(4-acetylphenyl)-3-(4-bromophenyloxy)pyrrolidine-2,5-dione
  参考文献：
  名称：

  N- （4-乙酰苯基）马来酰亚胺的芳香族醇容易迈克尔加成

  摘要：

  1-（4-乙酰基苯基）-3-芳氧基吡咯烷-2,5-二酮的一锅法，经济，有效的合成方法，一步一步即可完成，而且1-（4-乙酰基苯基）-吡咯-2的收率令人满意，5-二酮和芳香醇。所有化合物均通过物理，光谱和元素分析表征。

  DOI：

  10.1007/s11164-012-0932-z

文献信息

• Facile Michael-type addition of aromatic alcohols to N-(4-acetylphenyl)maleic imide
  作者：J. R. Patel、B. Z. Dholakiya

  DOI：10.1007/s11164-012-0932-z

  日期：2013.11

  economical, and efficient synthesis of 1-(4-acetylphenyl)-3-aryloxypyrrolidine-2,5-diones has been accomplished in single steps and in satisfactory yields from 1-(4-acetylphenyl)-pyrrole-2,5-diones and aromatic alcohols. All the compounds were characterized by physical, spectroscopic, and elemental analysis.

  1-（4-乙酰基苯基）-3-芳氧基吡咯烷-2,5-二酮的一锅法，经济，有效的合成方法，一步一步即可完成，而且1-（4-乙酰基苯基）-吡咯-2的收率令人满意，5-二酮和芳香醇。所有化合物均通过物理，光谱和元素分析表征。
• [EN] METHODS AND SYSTEMS FOR MODULATING HEPATIC GABA PRODUCTION OR RELEASE TO ALTER FOOD INTAKE IN MONOGASTRIC SPECIES<br/>[FR] PROCÉDÉS ET SYSTÈMES POUR MODULER LA PRODUCTION OU LA LIBÉRATION DE GABA HÉPATIQUE POUR MODIFIER L'APPORT ALIMENTAIRE CHEZ DES ESPÈCES MONOGASTRIQUES
  申请人：UNIV ARIZONA

  公开号：WO2021062048A2

  公开（公告）日：2021-04-01

  Methods and compositions (such as compounds, drugs, molecules, etc,) for modulating food intake, e.g., increasing food intake or reducing food intake, in a monogastric animal species. Certain methods herein feature administering to the animal a composition that depresses hepatic GABA production, depresses GABA release, inhibits expression or activity of GABA transaminase, inhibits expression or activity of particular GABA transporters associated with export of GABA, increases expression or activity of particular GABA transporters associated with GABA re- uptake, etc. The methods may help decrease food intake and subsequently improve weight loss. Certain methods herein may feature administering to the animal a composition that activates hepatic GABA production, activates GABA release, increases expression or activity of GABA transaminase, increases expression or activity of particular GABA transporters associated with export of GABA, decreases expression or activity of particular GABA transporters associated with GABA re-uptake, etc. The methods may help increase food intake, and subsequently help promote weight gain.
• [EN] METHODS AND COMPOSITIONS TO ALTER HEPATIC GABA RELEASE TO TREAT OBESITY-RELATED CONDITIONS<br/>[FR] PROCÉDÉS ET COMPOSITIONS POUR MODIFIER LA LIBÉRATION DE GABA HÉPATIQUE POUR TRAITER DES PROBLÈMES DE SANTÉ LIÉS À L'OBÉSITÉ
  申请人：UNIV ARIZONA

  公开号：WO2021203033A2

  公开（公告）日：2021-10-07

  Methods and compositions for treating conditions caused by altered hepatic GABA production and release, including hyperinsulinemia, insulin resistance, type II diabetes, obesity, and obesity-related conditions. The present invention describes hepatic GABA as a hepatokine. The methods herein feature manipulating the expression and/or activity of specific GABA transporters, e.g., increasing expression of SLC6A12 and/or SLC6A13 genes or increasing activity of the proteins for which they encode, BGT1 and/or GAT2; or decreasing expression of SLC6A6 and SLC6A8 genes or increasing the activity of the proteins for which they encode, TauT and/or CRT, which can increase hepatic GABA re-uptake or decrease hepatic GABA release to improve insulin sensitivity and prevent hypertension.
• In-vitro cytotoxicity, antioxidant, bleomycin-dependent DNA damage and immunomodulatory evaluation of 1-(4-acetylphenyl)-3-aryloxypyrrolidine-2, 5-dione based derivatives
  作者：Jigarkumar R. Patel、Bhaveshkumar D. Dhorajiya、Bharatkumar Z. Dholakiya、Farid A. Badria、Ahmed S. Ibrahim

  DOI：10.1007/s00044-014-0965-5

  日期：2014.8

  highest inhibitory antioxidant activity using ABTS methods. Compounds 5k, 5g, 5c, 5h, 5b, 5d, 5f, and 5j manifested the best protective effect against DNA damage induced by bleomycin. Moreover, an in-vitro cytotoxic activity evaluation of all synthesized compounds was against four cancer cell lines using 5-Fluorouracil as a standard anticancer drug.

  1-锅（1-乙酰-苯基）-3-芳氧基吡咯烷-2,5-二酮类衍生物5a-1的一锅，经济，有效的合成方法已经完成，一步合成1-（4-乙酰基苯基）的产率令人满意）-吡咯-2,5-二酮3和酚4a – l。所有化合物均通过物理，光谱和元素分析表征。生物测定的选择基于证明药物受体结合的概念。使用ABTS方法，化合物5g，5k，5h，5i，5a和5f表现出最高的抗氧化活性。化合物5k，5g，5c，5h，5b，5d，5f和5j对博来霉素诱导的DNA损伤表现出最佳的保护作用。此外，使用5-氟尿嘧啶作为标准抗癌药物，所有合成化合物的体外细胞毒性活性评估均针对四种癌细胞系。