2,5-dioxopyrrolidin-1-yl biphenyl-4-carboxylate | 299969-20-3

• 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: 2,5-dioxopyrrolidin-1-yl biphenyl-4-carboxylate
• 英文别名: p-phenylbenzoic acid N-hydroxysuccinimide ester；4-biphenylcarbonyl-N-hydroxysuccinimide ester；4-phenylbenzoic acid succinimide ester；biphenyl-4-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester；biphenyl-4-carboxylic acid 2,5-dioxopyrrolidin-1-yl ester；2,5-Dioxopyrrolidin-1-yl [1,1'-biphenyl]-4-carboxylate；(2,5-dioxopyrrolidin-1-yl) 4-phenylbenzoate
• CAS: 299969-20-3
• 化学式: C₁₇H₁₃NO₄
• 分子量: 295.295
• InChiKey: WPFNLWKQMSNEHE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  63.7
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2,5-dioxopyrrolidin-1-yl biphenyl-4-carboxylate 在 N,N-二异丙基乙胺 作用下， 生成 (S)-3-[(Biphenyl-4-carbonyl)-amino]-2-tert-butoxycarbonylamino-propionic acid methyl ester
  参考文献：
  名称：

  Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2

  摘要：

  Excitatory amino acid transporters (EAATs) play a pivotal role in maintaining glutamate homeostasis in the mammalian central nervous system, with the EAAT-2 subtype thought to be responsible for the bulk of the glutamate uptake in forebrain regions. A complete elucidation of the functional role of EAAT-2 has been hampered by the lack of potent and selective pharmacological tools. In this study, we describe the synthesis and biological activities of novel aryl-ether, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of EAAT-2. Compound (16) represents one of the most potent (IC50 = 85 +/- 5 nM) and selective inhibitors of EAAT-2 identified to date. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.08.003
• 作为产物：
  描述：

  N-羟基丁二酰亚胺 、 4-苯基苯甲酸 在 N,N'-二环己基碳二亚胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.08h， 以21.2%的产率得到2,5-dioxopyrrolidin-1-yl biphenyl-4-carboxylate
  参考文献：
  名称：

  肽指导的空心球形CoPt纳米颗粒超结构的合成与组装

  摘要：

  从“纳米”到“超级”：由结合有联苯单元尾部的钴结合肽组成的肽共轭物用于指导CoPt纳米粒子的空心球形超结构的合成和组装（见图）。这些可磁分离的上部结构表现出对甲醇氧化的电催化活性。

  DOI：

  10.1002/anie.201209910

文献信息

• [EN] MUSCARINIC AGONISTS<br/>[FR] AGONISTES MUSCARINIQUES
  申请人：LILLY CO ELI

  公开号：WO2004094363A1

  公开（公告）日：2004-11-04

  The present invention relates to compounds of Formula (I): which are agonists of the M-1 muscarinic receptor.

  本发明涉及以下式（I）的化合物，它们是M-1肌胆碱受体的激动剂。
• Preparation of 1-D nanoparticle superstructures with tailorable thicknesses using gold-binding peptide conjugates
  作者：Leekyoung Hwang、Chun-Long Chen、Nathaniel L. Rosi

  DOI：10.1039/c0cc02257h

  日期：——

  We describe the preparation of new 1-D gold nanoparticle superstructures with tailorable thicknesses formed using a self-assembled gold-binding peptide conjugate template and examine how the synthesis and assembly mechanism impacts the organization of the superstructures.

  我们描述了使用自组装的金结合肽结合物模板形成的具有可调节厚度的新的一维金纳米粒子超结构的制备，并研究了合成和组装机制如何影响超结构的组织。
• Modulation of intramolecular heterodimer-induced fluorescence quenching of tricarbocyanine dye for the development of fluorescent sensor
  作者：Tomoya Hirano、Jun Akiyama、Shuichi Mori、Hiroyuki Kagechika

  DOI：10.1039/c0ob00207k

  日期：——

  Various approaches have been used to modulate the fluorescence changes of sensors in the presence of target analytes, including intramolecular interaction between fluorophores or between fluorophore and other molecular species, like resonance energy transfer (RET). Here, we focus on fluorescence quenching by intramolecular heterodimer complex formation, which can be modulated over a shorter distance range than RET. We synthesized several conjugates of tricarbocyanine, which is a near-infrared fluorophore, with several quencher candidates via flexible short linker structure, and examined their fluorescence properties. Of our synthesized compounds, the dabcyl group proved to be the best quencher via heterodimer complex formation. The fluorescence of tricarbocyanine–dabcyl conjugates in aqueous media was almost completely quenched, and there was a dramatic fluorescence enhancement when heterodimer formation was blocked. These results suggested a design approach to develop fluorescence sensors for probing proximity relationships and structural transitions.

  各种方法被用来调节传感器在目标分析物存在时的荧光变化，包括荧光团之间或荧光团与其他分子物种之间的分子内作用力，例如共振能量转移（RET）。在这里，我们重点关注通过分子内异源二聚体复合物形成的荧光淬灭，这种方式的调节距离范围比RET更短。我们合成了几种三氰基钙调素的共轭物，这是一种近红外荧光团，与几种淬灭剂候选物通过灵活的短链结构结合，并检查了它们的荧光性质。在我们合成的化合物中，dabcyl基团通过异源二聚体复合物形成被证明是最佳淬灭剂。在水相介质中，三氰基钙调素–dabcyl共轭物的荧光几乎完全被淬灭，当异源二聚体形成被阻断时，荧光显著增强。这些结果暗示了一种设计方法，以开发用于探测近距离关系和结构转变的荧光传感器。
• Controlled Multi-functionalization Facilitates Targeted Delivery of Nanoparticles to Cancer Cells
  作者：Manish S. Hudlikar、Xiuru Li、Ivan A. Gagarinov、Nagesh Kolishetti、Margreet A. Wolfert、Geert-Jan Boons

  DOI：10.1002/chem.201503999

  日期：2016.1.22

  precision, thereby increasing the selectivity and potency of therapeutic drugs. A multifunctional nanoparticle is described for controlled conjugation of a cytotoxic drug, a cancer cell targeting ligand, and an imaging moiety. The approach is based on the chemical synthesis of polyethylene glycol that at one end is modified by a thioctic acid for controlled attachment to a gold core. The other end of the

  纳米医学的主要目标是以受控的方式将多个功能实体组合到单个纳米级设备中，以具有很高的空间精度靶向颗粒，从而提高治疗药物的选择性和效力。描述了一种多功能纳米颗粒，用于细胞毒素药物，癌细胞靶向配体和成像部分的可控偶联。该方法基于聚乙二醇的化学合成，该聚乙二醇的一端被硫辛酸修饰，可控地附着在金芯上。PEG聚合物的另一端被肼，胺或二苯并环辛炔醇部分改性，以分别与具有酮，活化酯或叠氮化物部分的功能实体结合。这种共轭方法通过应变促进的叠氮化物-炔烃环加成反应，通过酸不稳定的键控制阿霉素的受控附着，通过酰胺键控制Alexa Fluor染料的附着，以及B细胞细胞表面受体CD22的基于聚糖的配体。CD22配体的掺入通过受体介导的内吞作用导致纳米颗粒快速进入。阿通过键共价结合导致pH响应的阿霉素细胞内释放并显着增强纳米颗粒的细胞毒性。与非靶向纳米颗粒相比，CD22（+）淋巴瘤细胞的细胞毒性显着提高了60倍。使用
• Muscarinic agonists
  申请人：——

  公开号：US20040242584A1

  公开（公告）日：2004-12-02

  The present invention relates to compounds of Formula 1: Formula 1 which are agonists of the M-1 muscarinic receptor. 1

  本发明涉及公式1的化合物：公式1，它们是M-1肌动蛋白受体的激动剂。