2-[(5,6,7,8-Tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-4-ylhydrazinylidene)methyl]phenol | 300815-15-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并嘧啶酮衍生物
• 英文名称: 2-[(5,6,7,8-Tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-4-ylhydrazinylidene)methyl]phenol
• CAS: 300815-15-0
• 化学式: C₁₇H₁₆N₄OS
• 分子量: 324.406
• InChiKey: OWLSXQUCCNCTLB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  98.6
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-[(5,6,7,8-Tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-4-ylhydrazinylidene)methyl]phenol 在 lithium iodide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 24.0h， 以52%的产率得到3-(2-hydroxyphenyl)-8,9,10,11-tetrahydro[1]benzothieno[3,2-e][1,2,4]triazolo[4,3-c]pyrimidine
  参考文献：
  名称：

  Simple oxidation of pyrimidinylhydrazones to triazolopyrimidines and their inhibition of Shiga toxin trafficking

  摘要：

  The oxidative cyclisation of a range of benzothieno[2,3-d]pyrimidine hydrazones (7a-j) to the 1,2,4-triazolo[4,3-c]pyrimidines (8a-j) catalysed by lithium iodide or to the 1,2,4-triazolo[1,5-c]pyrimidines (10a-j) with sodium carbonate is presented. A complementary synthesis of the 1,2,4-triazolo[1,5-c]pyrimidines starting from the amino imine 11 is also reported. The effect of these compounds on Shiga toxin (STx) trafficking in HeLa cells and comparison to the previously reported Exo2 is also detailed (C) 2009 Elsevier Masson SAS. All rights reserved

  DOI：

  10.1016/j.ejmech.2009.10.007

文献信息

• Parkin ligase activation methods and compositions
  申请人：An2H Discovery Limited

  公开号：US10155936B2

  公开（公告）日：2018-12-18

  The present invention is directed to methods and compositions for activating a Parkin ligase by administering to a subject in need thereof a therapeutically effective amount of a compound that disrupts at least one Parkin ligase zinc finger. The present invention is also directed to methods of treating and/or reducing the incidence of diseases or conditions related to the activation of Parkin ligase.

  本发明涉及通过向有需要的受试者施用治疗有效量的破坏至少一个Parkin连接酶锌指的化合物来激活Parkin连接酶的方法和组合物。本发明还涉及治疗和/或降低与激活Parkin连接酶有关的疾病或病症发病率的方法。
• Methionine Aminopeptidase Inhibitors for Treating Infectious Diseases
  申请人：Olaleye Omonike Arike

  公开号：US20150141415A1

  公开（公告）日：2015-05-21

  The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.
• PARKIN LIGASE ACTIVATION METHODS AND COMPOSITIONS
  申请人：An2H Discovery Limited

  公开号：US20160160205A1

  公开（公告）日：2016-06-09

  The present invention is directed to methods and compositions for activating a Parkin ligase by administering to a subject in need thereof a therapeutically effective amount of a compound that disrupts at least one Parkin ligase zinc finger. The present invention is also directed to methods of treating and/or reducing the incidence of diseases or conditions related to the activation of Parkin ligase.
• Formulations of Methionine Aminopeptidase Inhibitors for Treating Infectious Diseases
  申请人：Olaleye Omonike A.

  公开号：US20170304288A1

  公开（公告）日：2017-10-26

  Provided herein are formulations and co-solvent formulations and methods for treating an infectious disease utilizing the same. The formulations and co-solvent formulations may comprise a hydroxyquinoline analog or its pharmaceutically acceptable salt, a solvent and at least two surfactants. Also provided are methods of quantitating a hydroxyquinoline analog in a sample via chromatographic/spectrometric measurements.
• [EN] METHIONINE AMINOPEPTIDASE INHIBITORS FOR TREATING INFECTIOUS DISEASES<br/>[FR] INHIBITEURS DE LA MÉTHIONINE AMINOPEPTIDASE POUR LE TRAITEMENT DE MALADIES INFECTIEUSES
  申请人：TEXAS SOUTHERN UNIVERSITY

  公开号：WO2015077057A1

  公开（公告）日：2015-05-28

  The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.