bis-[3]pyridylmethyl ether | 58418-69-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: bis-[3]pyridylmethyl ether
• 英文别名: 3,3'-(2-oxa-propane-1,3-diyl)-bis-pyridine；Bis-[3]pyridylmethyl-aether；3-(Pyridin-3-ylmethoxymethyl)pyridine
• CAS: 58418-69-2
• 化学式: C₁₂H₁₂N₂O
• 分子量: 200.24
• InChiKey: SKOHOWAOVMUZJY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  35
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] SELECTIVE NEURONAL NITRIC OXIDE SYNTHASE INHIBITORS<br/>[FR] INHIBITEURS SÉLECTIFS DES OXYDE NITRIQUE SYNTHASES NEURONALES
  申请人：UNIV NORTHWESTERN

  公开号：WO2021081528A1

  公开（公告）日：2021-04-29

  Disclosed are 7-phenyl-2-aminoquinoline compounds that are shown to inhibit the biological activity of neuronal nitric oxide synthases (nNOSs). Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds and pharmaceutical compositions for treating a subject in need thereof. Because the disclosed compounds are shown to inhibit the activity of neuronal nitric oxide synthases (nNOSs), the disclosed compounds and pharmaceutical compositions may be utilized in methods for treating a subject having or at risk for developing a disease or disorder that is associated with nNOS activity including neurological diseases and disorders.

  揭示了一种抑制神经一氧化氮合酶（nNOSs）生物活性的7-苯基-2-氨基喹啉化合物。还揭示了包含这些化合物的药物组合物，以及使用这些化合物和药物组合物治疗需要的主体的方法。由于这些揭示的化合物被证明可以抑制神经一氧化氮合酶（nNOSs）的活性，因此这些揭示的化合物和药物组合物可以用于治疗患有或有发展与nNOS活性相关的疾病或障碍的主体的方法，包括神经系统疾病和障碍。
• Luminescence-based methods and probes for measuring cytochrome P450 activity
  申请人：Promega Corporation

  公开号：US20040171099A1

  公开（公告）日：2004-09-02

  The present invention provides methods, compositions, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step methods using luminogenic molecules, e.g. luciferin or coelenterazines, that are cytochrome P450 substrates and that are also bioluminescent enzyme, e.g., luciferase, pro-substrates are provided. Upon addition of the luciferin derivative or other luminogenic molecule into a P450 reaction, the P450 enzyme metabolizes the molecule into a bioluminescent enzyme substrate, e.g., luciferin and/or luciferin derivative metabolite, in a P450 reaction. The resulting metabolite(s) serves as a substrate of the bioluminescent enzyme, e.g., luciferase, in a second light-generating reaction. Luminescent cytochrome P450 assays with low background signals and high sensitivity are disclosed and isoform selectivity is demonstrated. The present invention also provides an improved method for performing luciferase reactions which employs added pyrophosphatase to remove inorganic pyrophosphate, a luciferase inhibitor which may be present in the reaction mixture as a contaminant or may be generated during the reaction. The present method further provides a method for stabilizing and prolonging the luminescent signal in a luciferase-based assay using luciferase stabilizing agents such as reversible luciferase inhibitors.

  本发明提供了用于分析细胞、组织和动物代谢活性以及筛选化合物对细胞色素P450活性影响的方法、组成物、底物和试剂盒。特别地，提供了使用发光分子（如荧光素或发光虫菊素）的一步和两步方法，这些分子是细胞色素P450底物，也是生物发光酶（如荧光素酶）的前体底物。将荧光素衍生物或其他发光分子加入到P450反应中后，P450酶将这些分子代谢成生物发光酶底物（如荧光素和/或荧光素衍生物代谢物）的底物。产生的代谢物作为生物发光酶（如荧光素酶）的底物，在第二个发光反应中发光。揭示了低背景信号和高灵敏度的发光细胞色素P450测定方法，并证明了亚型选择性。本发明还提供了一种改进的荧光素酶反应方法，该方法采用添加焦磷酸酶以去除无机焦磷酸盐，该酶是可能存在于反应混合物中的污染物或在反应过程中生成的荧光素酶抑制剂。本方法进一步提供了一种使用可逆荧光素酶抑制剂等荧光素酶稳定剂稳定和延长荧光素酶基础测定中的发光信号的方法。
• LUMINOGENIC AND FLUOROGENIC COMPOUNDS AND METHODS TO DETECT MOLECULES OR CONDITIONS
  申请人：Promega Corporation

  公开号：US20140154716A1

  公开（公告）日：2014-06-05

  A method to detect the presence or amount of at least one molecule in a sample which employs a derivative of luciferin or a derivative of a fluorophore is provided. Compounds and compositions for carrying out the methods of the invention are also provided.

  本发明提供了一种检测样本中至少一种分子存在或数量的方法，该方法采用了luciferin的衍生物或荧光团的衍生物。还提供了用于执行本发明方法的化合物和组合物。
• LUMINESCENCE-BASED METHODS AND PROBES FOR MEASURING CYTOCHROME P450 ACTIVITY
  申请人：PROMEGA CORPORATION

  公开号：US20140380514A1

  公开（公告）日：2014-12-25

  The invention provides compounds, compositions, methods, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step methods using luminogenic molecules, e.g. luciferins or coelenterazines, that are cytochrome P450 substrates and that are also bioluminescent enzyme, e.g., luciferase, pro-substrates are provided. The present method further provides a method for stabilizing and prolonging the luminescent signal in a luciferase-based assay using luciferase stabilizing agents such as reversible luciferase inhibitors.

  本发明提供了化合物、组合物、方法、基质和工具，用于分析细胞、组织和动物中的代谢活性，并用于筛选测试化合物对细胞色素P450活性的影响。具体而言，提供了一步和两步方法，使用发光分子，例如荧光素或荧光素，它们是细胞色素P450底物，也是生物发光酶，例如荧光素酶，以及前体底物。本方法还提供了一种方法，使用可逆荧光素酶抑制剂等荧光素酶稳定剂稳定和延长荧光素酶基于荧光素的测定中的发光信号。
• Oxime derivatives as 5-lipoxygenase inhibitors
  申请人：ZENECA LIMITED

  公开号：EP0555068A1

  公开（公告）日：1993-08-11

  The invention concerns oxime derivatives of the formula I wherein R⁴ includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl; R⁵ includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl; Ar¹ is phenylene or a heteroaryl diradical; A¹ is a direct link to X¹, or A¹ is (1-4C)alkylene; X¹ is oxy, thio, sulphinyl or sulphonyl; Ar² is phenylene or a heteroaryl diradical; R¹ is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; and R² and R³ together form a group of the formula -A²-x²-A³- which together with the carbon atom to which A² and A³ are attached define a ring having 5 or 6 ring atoms, wherein each of A² and A³ is (1-3C)alkylene and X² is oxy, thio, sulphinyl, sulphonyl or imino; or a pharmaceutically-acceptable salt thereof; processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

  本发明涉及式 I 的肟衍生物 其中 R⁴包括氢、羧基、氨基甲酰基、氨基、氰基、三氟甲基、(1-4C)烷基氨基、二(1-4C)烷基氨基和(1-4C)烷基； R⁵ 包括氢、(1-4C)烷基、(3-4C)烯基、(3-4C)炔基、(2-5C)烷酰基、卤素-(2-4C)烷基和羟基-(2-4C)烷基； Ar¹ 是亚苯基或二元杂芳基； A¹ 是与 X¹ 的直接连接，或 A¹ 是（1-4C）亚烷基； X¹ 是氧基、硫代、亚砜基或磺酰基； Ar² 是亚苯基或二元杂芳基； R¹ 是(1-4C)烷基、(3-4C)烯基或(3-4C)炔基；以及 R² 和 R³ 一起形成式 -A²-x²-A³- 的基团，该基团与 A² 和 A³ 所连接的碳原子一起定义了一个具有 5 或 6 个环原子的环，其中 A² 和 A³ 均为 (1-3C)亚烷基，X² 为氧基、硫代、亚砜基、磺酰基或亚氨基； 或其药学上可接受的盐； 它们的制造工艺；含有它们的药物组合物及其作为 5-脂氧合酶抑制剂的用途。