N-（2-氨基苯甲酰基）甘氨酸 | 526-21-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-（2-氨基苯甲酰基）甘氨酸
• 中文别名: 2-氨基马尿酸
• 英文名称: N-(2-aminobenzoyl)-glycine
• 英文别名: N-(2-Aminobenzoyl)glycine；o-aminohippuric acid；2-Aminohippursaeure；H₂N-Abz-Gly-OH；N-anthraniloyl-glycine；N-Anthraniloyl-glycin；2-Aminohippuric acid；2-[(2-aminobenzoyl)amino]acetic acid
• CAS: 526-21-6
• 化学式: C₉H₁₀N₂O₃
• mdl: MFCD07345519
• 分子量: 194.19
• InChiKey: DEFPNMKDESPGBA-UHFFFAOYSA-N

物化性质

• 熔点：
  327 °C
• 沸点：
  498.1±30.0 °C(Predicted)
• 密度：
  1.356±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.111
• 拓扑面积：
  92.4
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 海关编码：
  2924299090

反应信息

• 作为反应物：
  描述：

  N-（2-氨基苯甲酰基）甘氨酸 反应 6.0h， 生成 (4-氧代-3(4H)-喹唑啉基)乙酸
  参考文献：
  名称：

  Chinazolincarbonsäuren。七。米特隆。Ein einfacher Zugang zu（4-Oxo-3,4-dihydrochinazolin-3-yl）-alkansäuren，（4-Oxo-3,4-dihydro-1,2,3-benzotriazin-3-yl）-alkansäurenund deren Estern †

  摘要：

  喹唑啉羧酸。轻松合成（4-Oxo-3,4-dihydroquinazolin-3-yl）-链烷酸，（4-Oxo-3,4-dihydro-1,2,3-3-苯并三嗪-3-基）-链烷酸和他们的酯

  DOI：

  10.1002/hlca.19850680410
• 作为产物：
  描述：

  邻硝基苯甲酸 在 palladium on activated charcoal 草酰氯 、 氢气 、 三乙胺 、 N,N-二甲基甲酰胺 作用下， 以 四氢呋喃 、 乙醇 、 水 为溶剂， 反应 23.0h， 生成 N-（2-氨基苯甲酰基）甘氨酸
  参考文献：
  名称：

  Neutral, acidic, and basic derivatives of anthranilamide that confer different formal charge to reducing oligosaccharides

  摘要：

  To facilitate the use of oligosaccharides as analytical tools in biological studies, we have designed, synthesized, and conjugated to maltosaccharides a novel series of homologous small fluorescent moieties that differ in formal charge. These moieties are amide derivatives of anthranilic acid: uncharged N-(2-aminobenzoyl)glycinamide (ABGlyAmide; 2), acidic N,N-dimethyl-N'-(2-aminobenzoyl)ethylenediamine (ABGlyDIMED; 3), and basic N-(2-aminobenzoyl)glycine (ABGly; 1). Routes for synthesis and optimal reaction conditions for glycoconjugation by conventional reductive amination are presented, as is the compatibility of these adducts with common analytical and preparative chromatographic methods, including RP-HPLC and HPAEC-PAD. These novel anthranilic acid derivatives confer both fluorescence and defined charge to oligosaccharides, and so enhance the repertoire of chromatographic and analytical methods for which anthranilic acid can be used. Furthermore, because glucosaccharides have rigid solution structure, these small fluorescent adducts with different formal charge are ideal tools for molecular sizing studies of membrane pores. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.carres.2003.10.020

文献信息

• Non-peptidic inhibitors of human neutrophil elastase: The design and synthesis of sulfonanilide-containing inhibitors
  作者：Katsuhiro Imaki、Takanori Okada、Yoshisuke Nakayama、Yuuki Nagao、Kaoru Kobayashi、Yasuhiro Sakai、Tetsuya Mohri、Takaaki Amino、Hisao Nakai、Masanori Kawamura

  DOI：10.1016/s0968-0896(96)00216-7

  日期：1996.12

  A novel series of pivaloyloxy benzene derivatives has been identified as potent and selective human neutrophil elastase (HNE) inhibitors. Convergent syntheses were developed in order to identify the inhibitors which are intravenously effective in an animal model. A compound of particular interest is the sulfonanilide-containing analogues. Structure-activity relationships are discussed. Structural requirements

  已经鉴定出一系列新的新戊酰氧基苯衍生物作为有效的和选择性的人中性粒细胞弹性蛋白酶（HNE）抑制剂。为了确定在动物模型中静脉内有效的抑制剂，开发了收敛合成法。特别感兴趣的化合物是含磺酰苯胺的类似物。讨论了构效关系。还讨论了代谢稳定的结构要求。
• F-18 RADIOLABELED COMPOUNDS FOR DIAGNOSING AND MONITORING KIDNEY FUNCTION
  申请人：KASINA LAILA INNOVA PHARMACEUTICALS PRIVATE LIMITED

  公开号：US20140086837A1

  公开（公告）日：2014-03-27

  The invention relates to 18 F-labeled compounds of formula (I), hydrates, isomers, or pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions. The invention relates to the methods of diagnosing kidney function in humans by PET imaging.

  这项发明涉及到式(I)的18F标记化合物，以及它们的水合物、异构体或药学上可接受的盐，以及它们的制备方法和药物组合物。该发明涉及通过PET成像诊断人类肾功能的方法。
• METHODS AND SYSTEMS FOR DESIGNING AND/OR CHARACTERIZING SOLUBLE LIPIDATED LIGAND AGENTS
  申请人：TUFTS MEDICAL CENTER

  公开号：US20160052982A1

  公开（公告）日：2016-02-25

  The present application provides methods for preparing soluble lipidated ligand agents comprising a ligand entity and a lipid entity, and in some embodiments, provides relevant parameters of each of these components, thereby enabling appropriate selection of components to assemble active agents for any given target of interest.

  本申请提供了制备可溶性脂质化配体药剂的方法，包括配体实体和脂质实体，并在某些实施例中提供了这些组分的相关参数，从而使得能够适当选择组分来组装出针对任何感兴趣的靶点的活性药剂。
• [EN] TARGETED DELIVERY TO BETA CELLS<br/>[FR] ADMINISTRATION CIBLÉE À DES CELLULES BÊTA
  申请人：CHOUDHARY AMIT

  公开号：WO2018195486A1

  公开（公告）日：2018-10-25

  The disclosure includes zinc prodrugs for targeted delivery of therapeutic, diagnostic or imaging agents to β-cells and methods of use therefor. The disclosure also includes targeted delivery of small molecules to β-cells that stabilize and activate CRISPR effector proteins comprising at least one destabilization domain, to enable CRISPR-based genome editing and transcriptional activation or repression in β-cells.

  本公开内容包括用于将治疗性、诊断性或成像剂靶向递送至β细胞的锌前药及其使用方法。本公开内容还涉及将小分子靶向递送至β细胞，这些小分子能够稳定并激活至少含有一个不稳定域的CRISPR效应蛋白，从而在β细胞中实现基于CRISPR的基因编辑和转录激活或抑制。
• [EN] POLYMERIC HYPERBRANCHED CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS POLYMÉRIQUES HYPERBRANCHÉS
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024048A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I),wherein POL is a polymeric moiety,each Hyp is independently a hyperbranched moiety,each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water- soluble carrier-linked prodrugs and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为（I），其中POL是聚合物基团，每个Hyp是独立的超支化基团，每个基团SP是独立的间隔基团，每个L是独立的可逆前药连接基团，m为0或1，每个n是独立的整数，范围从2到200，每个x是独立的0或1。此外，还涉及包含所述水溶性载体连接的前药的药物组合物和治疗方法。