4-叠氮基苯甲酰肼 | 63296-32-2

• 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: 4-叠氮基苯甲酰肼
• 英文名称: p-Azidobenzoyl hydrazide
• 英文别名: azidobenzoyl hydrazide；4-azidobenzohydrazide；Benzoic acid, 4-azido-, hydrazide
• CAS: 63296-32-2
• 化学式: C₇H₇N₅O
• mdl: MFCD00083160
• 分子量: 177.165
• InChiKey: YRLKXQVDEQEYSN-UHFFFAOYSA-N

物化性质

• 熔点：
  169-170°C
• 溶解度：
  可溶于DMSO（少许）、甲醇（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  69.5
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-叠氮基苯甲酰肼 在 4-二甲氨基吡啶 、 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， 反应 4.33h， 以5%的产率得到N-(4-azidobenzohydrazide)gambogamide
  参考文献：
  名称：

  Derivatives of gambogic acid and analogs as activators of caspases and inducers of apoptosis

  摘要：

  本发明涉及新的甘黄酸衍生物及其类似物。本发明还涉及发现，新的甘黄酸衍生物是半胱氨酸蛋白酶的激活剂和凋亡诱导剂。因此，本发明的半胱氨酸蛋白酶激活剂和凋亡诱导剂可用于诱导细胞死亡，在各种临床病况中，异常细胞的无序生长和传播。

  公开号：

  US20070093456A1
• 作为产物：
  描述：

  tert-butyl 2-(4-azidobenzoyl)hydrazine carboxylate 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 4-叠氮基苯甲酰肼
  参考文献：
  名称：

  Biodegradable Magnetic Nanocarrier for Stimuli Responsive Drug Release

  摘要：

  Biocompatible nanocarriers conjugated with magnetic nanoparticle, doxorubicin and poly(ethylene oxide) (PEG) motif have been designed (PVLPEG-PVLDOXI-PCL-PHOS) to create a magnetic vector under magnetic field. Acylhydrazine linker is used to release the drug exactly at the mild acidic conditions resembling the pH of the cancerous cells. All the monomers and polymers are characterized carefully by the routine analytical techniques. Thermogravimetric analysis (TGA), FT-IR spectroscopy and scanning electron microscope (SEM) techniques are employed to confirm the anchoring of iron particle (Fe3O4) to the PVLPEG-PVLDOXI-PCL-PHOS. Reservoir capabilities of the newly designed biodegradable nanocarrier are tested by both dynamic light scattering (DLS) and transmission electron microscopy (TEM). Drug release profile from nanocarrier is monitored by fluorimeter. The release profile shows the importance of having the acylhydrazine linker that helps to release the drug at the mild acidic conditions similar to cancerous cells. Confocal laser scanning microscopy (CLSM) and flow cytometry studies on 4T cells indicate that nanocarriers from PVLPEG-PVLDOXI-PCL-PHOS polymer are internalized efficiently. It is very interesting to note that the nanocarriers have exhibited both biologically and magnetically targeting abilities toward 4T cells in vitro.

  DOI：

  10.1021/ma500384m

文献信息

• [EN] POLYPEPTIDE-OPIOID CONJUGATES AND USES THEREOF<br/>[FR] CONJUGUÉS POLYPEPTIDES OPIOÏDES ET UTILISATIONS ASSOCIÉES
  申请人：ANGIOCHEM INC

  公开号：WO2013056096A1

  公开（公告）日：2013-04-18

  The invention features polypeptide-opioid conjugates capable of crossing the blood-brain barrier. The polypeptide-opioid conjugates can be used to treat a condition that is modulated by opioid receptors such as pain (e.g., postoperative pain, cancer pain, acute pain, and chronic pain).

  这项发明涉及能够穿越血脑屏障的多肽-阿片类肽共轭物。这些多肽-阿片类肽共轭物可用于治疗受阿片类受体调节的疾病，如疼痛（例如术后疼痛、癌症疼痛、急性疼痛和慢性疼痛）。
• [EN] BORONATE-MEDIATED DELIVERY OF MOLECULES INTO CELLS<br/>[FR] ADMINISTRATION DE MÉDICAMENT MÉDIÉE PAR LES BORONATE
  申请人：WISCONSIN ALUMNI RES FOUND

  公开号：WO2013110005A1

  公开（公告）日：2013-07-25

  Methods for enhancing cellular uptake of cargo molecules by boronating the cargo molecule, particularly with one or more phenylboronic acid groups. Cellular uptake includes at least partial uptake into the cytosol. Boronation includes ligating, crosslinking or otherwise bonding one or more phenylboronic acids substituted to contain a reactive group to a cargo molecule. Boronation also includes ligating, crosslinking or otherwise bonding a phenylboronated oligopeptide to a cargo molecule. The phenylboronate groups are optionally conjugated to the cargo molecule via linking moieties that can be selectively cleaved. The invention includes certain phenylboronates which are boronation reagents, certain boronated oligopeptides and certain boronated peptides and proteins. The invention also includes kits for enhancing cellular uptake of cargo molecules by boronation with one or more phenylboronates or boronated oligopeptides.

  增强货物分子细胞摄取的方法，通过将货物分子硼酸化，特别是与一个或多个苯硼酸基团硼酸化。细胞摄取至少包括部分摄取到细胞质中。硼酸化包括将一个或多个含有反应基团的取代苯硼酸与货物分子连接、交联或以其他方式键合。硼酸化还包括将苯硼酸化的寡肽与货物分子连接、交联或以其他方式键合。可选地，苯硼酸基团通过可以选择性切割的连接基团与货物分子连接。本发明包括某些作为硼酸化试剂的苯硼酸、某些硼酸化的寡肽以及某些硼酸化的肽和蛋白质。本发明还包括通过用一种或多种苯硼酸或硼酸化寡肽硼酸化来增强货物分子细胞摄取的试剂盒。
• [EN] NUCLEIC ACID-POLYPEPTIDE COMPOSITIONS AND USES THEREOF<br/>[FR] COMPOSITIONS D'ACIDE NUCLÉIQUE-POLYPEPTIDE ET UTILISATIONS DE CELLES-CI
  申请人：AVIDITY BIOSCIENCES LLC

  公开号：WO2019071028A1

  公开（公告）日：2019-04-11

  Disclosed herein are compositions and pharmaceutical formulations that comprise a binding moiety conjugated to a modified polynucleic acid molecule and a polymer. Also described herein include methods for treating a cancer which utilize a composition or a pharmaceutical formulation comprising a binding moiety conjugated to a polynucleic acid molecule and a polymer.

  本文披露了包含与修饰的多核苷酸分子和聚合物结合基团的组合物和药物配方。本文还描述了利用包含与多核苷酸分子和聚合物结合基团共轭的组合物或药物配方治疗癌症的方法。
• BIFUNCTION CHEMICAL EPIGENENTIC MODIFIERS AND METHODS OF USE
  申请人：The University of North Carolina at Chapel Hill

  公开号：US20210355476A1

  公开（公告）日：2021-11-18

  The present disclosure relates to bifunctional chemical epigenetic modifiers, and methods of making, kits and using the bifunctional chemical epigenetic modifiers. The bifunctional chemical epigenetic modifiers can include a FK506 molecule or derivative thereof, a linker and a bifunctional ligand. The bifunctional ligand can be a histone deacetylase inhibitor.

  本公开涉及双功能化学表观遗传修饰剂，以及制备方法、工具包和使用双功能化学表观遗传修饰剂的方法。双功能化学表观遗传修饰剂可以包括FK506分子或其衍生物，连接剂和双功能配体。双功能配体可以是组蛋白去乙酰化酶抑制剂。
• ALKYNE PHOSPHORAMIDITES AND PREPARATION OF SPHERICAL NUCLEIC ACID CONSTRUCTS
  申请人：NORTHWESTERN UNIVERSITY

  公开号：US20160159834A1

  公开（公告）日：2016-06-09

  The present disclosure is directed to compositions comprising alkyne oligonucleotides, nanoconjugates prepared from the same, and methods of their use.

  本文揭示了包含炔基寡核苷酸的组合物、由其制备的纳米共轭物以及它们的使用方法。