p-aminophenylguanidine | 18905-24-3

• 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: p-aminophenylguanidine
• 英文别名: (4-amino-phenyl)-guanidine；(4-Amino-phenyl)-guanidin；1-(4-aminophenyl)guanidine；N-(4-Aminophenyl)guanidine；2-(4-aminophenyl)guanidine
• CAS: 18905-24-3
• 化学式: C₇H₁₀N₄
• mdl: MFCD12024864
• 分子量: 150.183
• InChiKey: HXKWSIPCTVYMBN-UHFFFAOYSA-N

物化性质

• 沸点：
  312.3±44.0 °C(Predicted)
• 密度：
  1.34±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  90.4
• 氢给体数：
  3
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  p-aminophenylguanidine 在 AurF-R₉₆E/T₁₀₀A/L₂₀₂F 作用下， 生成 N-4-硝基苯基胍
  参考文献：
  名称：

  Structural and biochemical basis for the firm chemo- and regioselectivity of the nitro-forming N-oxygenase AurF

  摘要：

  基于硫链丝菌素黄素（Streptomyces thioluteus）中硝基形成单加氧酶AurF的晶体结构进行的定点诱变研究表明，AurF变体能够选择性地将胍基和脒基取代的苯胺转化为相应的硝基化合物。我们的结果为位选择性N-氧化提供了新的生化依据。

  DOI：

  10.1039/c0cc02811h
• 作为产物：
  描述：

  (4-acetylamino-phenyl)-guanidine; hydrochloride 在 盐酸 作用下， 生成 p-aminophenylguanidine
  参考文献：
  名称：

  Miller, Journal of the Chemical Society, 1949, p. 2722

  摘要：

  DOI：

文献信息

• Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors
  作者：Xiaoxia Hu、Hui Zhao、Youzhi Wang、Zhan Liu、Bainian Feng、Chunlei Tang

  DOI：10.1016/j.bmcl.2018.08.035

  日期：2018.11

  kinase 2 (CDK2) is a promising target for various diseases such as cerebral hypoxia, cancer, and neurodegenerative diseases. Here we reported the structure-based synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as CDK2 inhibitors, which exhibited potent CDK2 inhibitory activities, as well as anticancer activities in low concentration against two human cancer

  作为丝氨酸/苏氨酸激酶，细胞周期蛋白依赖性激酶2（CDK2）是各种疾病（如脑缺氧，癌症和神经退行性疾病）的有希望的靶标。在这里我们报道了作为CDK2抑制剂的新型5,6-二氢嘧啶基[4,5- f ]喹唑啉衍生物的结构化合成和生物学评估，该化合物表现出有效的CDK2抑制活性，以及​​低浓度时对两种人类癌症的抗癌活性。细胞系（MCF-7和HCT116）。尤其是，化合物11a和11f（对于CDK2的IC 50值分别为0.11和0.09μM）已显示出对CDK2的显着抑制作用，并且对MCF-7和HCT116细胞系显示出极大的抑制活性。
• COMPOUND HAVING AZO SKELETON, PIGMENT DISPERSANT, PIGMENT COMPOSITION, PIGMENT DISPERSION, AND TONER
  申请人：CANON KABUSHIKI KAISHA

  公开号：US20160208106A1

  公开（公告）日：2016-07-21

  A compound that improves the dispersibility of pigments in non-water-soluble solvents is provided. A pigment dispersant, a pigment composition, a pigment dispersion, and a toner in which this compound is used are also provided. This compound has a polymer and a monoazo compound having a certain structure binding to each other. The pigment dispersant, the pigment composition, the pigment dispersion, and the toner contain this compound.

  提供了一种可以改善颜料在非水溶性溶剂中分散性的化合物。还提供了一种颜料分散剂、颜料组合物、颜料分散液和使用了这种化合物的色调剂。该化合物包含聚合物和一种具有特定结构的单偶氮化合物相互结合。颜料分散剂、颜料组合物、颜料分散液和色调剂均含有这种化合物。
• GUANIDINE BASED COMPOUNDS
  申请人：Rozas Hernando Maria Isabel

  公开号：US20100331384A1

  公开（公告）日：2010-12-30

  The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into α and β subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel guanidine and 2-aminoimidazoline compounds which are ligands of the alpha2-adrenoceptor (α2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of α2-ARs associated disorders, such as depression, schizophrenia, glaucoma and analgesia.

  肾上腺素受体或肾上腺素受体是一类G蛋白偶联受体家族，分为α和β亚类。肾上腺素受体在调节多种生理条件中起着重要作用，其功能失调已被认为与多种疾病的病理生理有关。本文披露了一系列新型胍啶和2-氨基咪唑啉化合物，它们是肾上腺素受体的α2-亚型（α2-ARs）亚类的配体。该发明还提供了包含这些新型化合物的药物组合物。这些化合物适用于制造用于治疗与α2-ARs相关疾病的药物，如抑郁症、精神分裂症、青光眼和镇痛的药物。
• [DE] SELEKTIVE INHIBITOREN DES UROKINASE-PLASMINOGEN AKTIVATORS<br/>[EN] SELECTIVE INHIBITORS OF THE UROKINASE PLASMINOGENE ACTIVATORS<br/>[FR] INHIBITEURS SELECTIFS DE L'ACTIVATEUR DE L'UROKINASE PLASMINOGENE
  申请人：WILEX BIOTECHNOLOGY GMBH

  公开号：WO2001014324A1

  公开（公告）日：2001-03-01

  Die vorliegende Erfindung betrifft neue selektive Inhibitoren des Urokinase-Plasminogenaktivators (uPA, EC 3.4.21.31) vom Arylguanidintyp.

  这项发明涉及新的芳基胍类选择性尿激酶-纤溶酶原激活剂（uPA，EC 3.4.21.31）抑制剂。
• Potassium channel blocking agents
  申请人：NeuroSearch A/S

  公开号：US20020049246A1

  公开（公告）日：2002-04-25

  This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, in particular asthma, cystic fibrosis, chronic obstructive pulmonary disease and rhinorrhea, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhoea, ischaemia, cerebral ischaemia, ischaemic hearth disease, angina pectoris, coronary hearth disease, traumatic brain injury, psychosis, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labor, baldness, cancer, and immune suppression.

  本发明涉及新型钾通道阻滞剂及其在制备药物组合物中的应用。此外，本发明还涉及用于治疗或缓解与钾通道活性有关的疾病或疾病的药物组合物，特别是哮喘、囊性纤维化、慢性阻塞性肺疾病和流涕、惊厥、血管痉挛、冠状动脉痉挛、肾脏疾病、多囊肾病、膀胱痉挛、尿失禁、膀胱出流道梗阻、肠易激综合征、胃肠功能障碍、分泌性腹泻、缺血、脑缺血、缺血性心脏病、心绞痛、冠心病、创伤性脑损伤、精神病、焦虑、抑郁症、痴呆、记忆和注意力缺陷、阿尔茨海默病、痛经、嗜睡病、雷诺氏病、间歇性跛行、Sjorgren综合征、偏头痛、心律失常、高血压、失神发作、肌萎缩性肌肉营养不良、干口症、2型糖尿病、高胰岛素血症、早产、秃发、癌症和免疫抑制。