(E)-2-(2-methoxybenzylidene)hydrazine-1-carboximidamide | 42452-51-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: (E)-2-(2-methoxybenzylidene)hydrazine-1-carboximidamide
• 英文别名: (2-methoxy-benzylidenamino)-guanidine；(2-Methoxy-benzylidenamino)-guanidin；N-[(E)-[(2-Methoxyphenyl)methylidene]amino]guanidine；2-[(E)-(2-methoxyphenyl)methylideneamino]guanidine
• CAS: 42452-51-7
• 化学式: C₉H₁₂N₄O
• 分子量: 192.22
• InChiKey: NWNHXWIPOLXCLG-WUXMJOGZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  86
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  邻甲氧基苯甲醛 、 氨基胍媒染剂 生成 (E)-2-(2-methoxybenzylidene)hydrazine-1-carboximidamide
  参考文献：
  名称：

  Grammaticakis, Bulletin de la Societe Chimique de France, 1952, p. 446,453

  摘要：

  DOI：

文献信息

• Gram‐Positive and Gram‐Negative Antibiotic Activity of Asymmetric and Monomeric Robenidine Analogues
  作者：Cecilia C. Russell、Andrew Stevens、Hongfei Pi、Manouchehr Khazandi、Abiodun D. Ogunniyi、Kelly A. Young、Jennifer R. Baker、Siobhann N. McCluskey、Stephen W. Page、Darren J. Trott、Adam McCluskey

  DOI：10.1002/cmdc.201800463

  日期：2018.12.6

  except with concomitant introduction of an imine C‐alkyl group. The activity of these analogues against MRSA and VRE ranged from 8 μg mL−1 to inactive (MIC>128 μg mL−1) with the naphthyl and indole analogues. Gram‐negative activity was most promising with two compounds at 16 μg mL−1 against E. coli. Against P. aeruginosa, the highest activity observed was with MIC values of 32 μg mL−1 with another two analogues

  罗非替丁的去对称化（1：N '，2-二（（E）-4-氯苄叉）肼-1-羧酰亚胺肼）和亚胺烷基取代基的引入具有良好的抗生素活性。值得注意的是，两种类似物对耐万古霉素的肠球菌（VRE）的效力有所提高，其中一种的MIC为0.5μgmL -1。发现有五个类似物比铅1具有更强的效价。吲哚部分的引入导致针对甲氧西林抗性金黄色葡萄球菌（MRSA）的活性最强的robenidine类似物，MIC为1.0μgmL -1。亚胺C = NH等位基因（C = O / C = S）不活跃。单体类似物为16–64μgmL-1对MRSA和VRE有效。缺少末端酰肼NH部分的类似物在64μgmL -1下显示适度的革兰氏阴性活性。研究表明，在16–64μgmL -1下， 4-叔丁基类似物对革兰氏阳性和阴性菌株均具有活性。通常，除伴随引入亚胺C-烷基外，对芳香族基团的其他修饰耐受性差。这些类似物对MRSA和VRE的活性范围为8μgmL
• [EN] NOVEL THERAPEUTIC USES OF BENZYLIDENEGUANIDINE DERIVATIVES FOR THE TREATMENT OF PROTEOPATHIES<br/>[FR] NOUVELLES UTILISATIONS THÉRAPEUTIQUES DE DÉRIVÉS DE LA BENZYLIDÈNE-GUANIDINE DANS LE TRAITEMENT DE PROTÉOPATHIES
  申请人：INFLECTIS BIOSCIENCE

  公开号：WO2016001389A1

  公开（公告）日：2016-01-07

  The present invention relates to novel uses of a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, in treating a disorder associated with the PPP1R15A pathway and associated with protein misfolding stress and in particular with accumulation of misfolded proteins selected in the group of tauopathies, synucleinopathies, polyglutamine and polyalanine diseases, leukodystrophies, cystic fibrosis, multiple sclerosis, lysosomal storage disorders, amyloidosis diseases, inflammation, metabolic disorders, cardio-vascular disorders, osteoporosis, nervous system trauma, ischemia.

  本发明涉及一种化合物（I）的新用途，或其互变异构体和/或药用盐，在治疗与PPP1R15A途径相关的紊乱，与蛋白质错误折叠应激相关，特别是与在tau病、α-突触核蛋白病、多聚谷氨酸和多聚丙氨酸疾病、白质病、囊性纤维化、多发性硬化、溶酶体贮积疾病、淀粉样变性疾病、炎症、代谢紊乱、心血管疾病、骨质疏松症、神经系统创伤、缺血等相关的错误折叠蛋白的积累。
• [EN] GUANIDINE DERIVATIVES AND THEIR USE IN THE PRODUCTION OF A MEDICAMENT FOR BLOCKING XANTHINE OXIDASE/DEHYDROGENASE<br/>[FR] DERIVES DE GUANIDINE ET LEUR UTILISATION DANS LA PRODUCTION D'UN MEDICAMENT DESTINE A BLOQUER LES XANTHINE OXYDASES/DESHYDROGENASES
  申请人：MELACURE THERAPEUTICS AB

  公开号：WO2001025192A1

  公开（公告）日：2001-04-12

  The present invention relates to guanidine derivatives and pharmaceutically acceptable acid salts thereof. The invention further relates to pharmaceutical preparations containing said compounds, and the use of said compounds for treatment of any type of condition where the expression of xanthine oxidase/xanthine dehydrogenase enzymes is involved. The invention particularly relates to the use of these compounds in the preparation of a medicament for enhancing the survical of a transplanted cell, organ or tissue, or cell, organ or tissue to be transplanted.

  本发明涉及胍衍生物及其药用酸盐。本发明还涉及含有该化合物的制药制剂，以及使用该化合物治疗涉及黄嘌呤氧化酶/黄嘌呤脱氢酶酶表达的任何类型疾病的用途。本发明特别涉及使用这些化合物制备增强移植细胞、器官或组织的存活或待移植的细胞、器官或组织的药物。
• Therapeutic uses of benzylideneguanidine derivatives for the treatment of proteopathies
  申请人：InFlectis BioScience

  公开号：US10709677B2

  公开（公告）日：2020-07-14

  The present invention relates to novel uses of a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, in treating a disorder associated with the PPP1R15A pathway and associated with protein misfolding stress and in particular with accumulation of misfolded proteins selected in the group of tauopathies, synucleinopathies, polyglutamine and polyalanine diseases, leukodystrophies, cystic fibrosis, multiple sclerosis, lysosomal storage disorders, amyloidosis diseases, inflammation, metabolic disorders, cardio-vascular disorders, osteoporosis, nervous system trauma, ischemia.

  本发明涉及式（I）化合物或其同系物和/或其药学上可接受的盐在治疗与 PPP1R15A 通路相关且与蛋白质错误折叠应激相关的疾病中的新用途，特别是与选自牛磺酸病、多谷氨酰胺和多丙氨酸疾病、白质营养不良、囊性纤维化、多发性硬化症、溶酶体贮存疾病、淀粉样变性疾病中的错误折叠蛋白质累积相关的疾病中的新用途、突触核蛋白病、多谷氨酰胺和多丙氨酸疾病、白质营养不良、囊性纤维化、多发性硬化、溶酶体贮存紊乱、淀粉样变性疾病、炎症、代谢紊乱、心血管疾病、骨质疏松症、神经系统创伤、缺血。
• Self-assembled active agents
  申请人：The United States of America, as represented by the Secretary of Agriculture

  公开号：US11166464B2

  公开（公告）日：2021-11-09

  A self-assembled active agent may be formed by a process including covalently bonding at least a first component molecule and a second component molecule, the two component molecules displaying synergy such that the effective amount of the self-assembled active agent is lower than the sum of the effective amounts of the first component molecule and the second component molecule. The component molecules may be chosen such that the covalent bonding is reversible, for example through a hydrazone bond between an amine and an aldehyde. The active agent may thus have controllable activity such as an antimicrobial agent, a biocide, an antiviral agent, a preservative, an antifouling agent, a disinfectant, or a sensor agent, such as for a particular molecule or for pH.

  自组装活性剂可通过一种工艺形成，该工艺包括至少共价键合第一组分分子和第二组分分子，这两种组分分子显示出协同作用，从而使自组装活性剂的有效量低于第一组分分子和第二组分分子的有效量之和。可以选择共价键可逆的组分分子，例如通过胺和醛之间的腙键。因此，活性剂可具有可控活性，如抗菌剂、杀菌剂、抗病毒剂、防腐剂、防污剂、消毒剂或传感剂，如针对特定分子或 pH 值的传感剂。