4-(2-吡嗪基)苯酚 | 108030-86-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 中文名称: 4-(2-吡嗪基)苯酚
• 中文别名: 4-吡嗪-2-基-苯酚
• 英文名称: 2-(4-hydroxyphenyl)pyrazine
• 英文别名: 4-(pyrazin-2-yl)phenol；(4-hydroxyphenyl)pyrazine；4-pyrazin-2-ylphenol
• CAS: 108030-86-0
• 化学式: C₁₀H₈N₂O
• 分子量: 172.186
• InChiKey: PNSWNYYMDRNEFB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  46
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  4-(2-吡嗪基)苯酚 在 potassium carbonate 、 三氟乙酸 作用下， 以 乙腈 为溶剂， 反应 8.5h， 生成 2-formyl-4-(pyrazin-2-yl)phenyl trifluoromethanesulfonate
  参考文献：
  名称：

  [EN] COMPOSITIONS FOR THE TREATMENT OF PULMONARY FIBROSIS
  [FR] COMPOSITIONS POUR LE TRAITEMENT D'UNE FIBROSE PULMONAIRE

  摘要：

  本发明涉及化合物及其在预防及/或治疗肺纤维化及/或相关病症的应用。

  公开号：

  WO2018018091A1
• 作为产物：
  描述：

  2-(4-甲氧基苯基)吡嗪 在 吡啶盐酸盐 作用下， 反应 1.0h， 以88%的产率得到4-(2-吡嗪基)苯酚
  参考文献：
  名称：

  Synthesis and in vitro evaluation of botryllazine B analogues as a new class of inhibitor against human aldose reductase

  摘要：

  Botryllazine B analogues of diverse substitution patterns have been prepared, and their in vitro inhibitory activities against recombinant human aldose reductase (h-ALR2) evaluated. Among the 15 compounds tested, 6-(4-aminophenyl)-2-(4-hydroxyphenyl)carbonylpyrazine (7b) proved to be the most potent inhibitor, with IC50=0.91 mu M. Kinetic analyses of 7b and botryllazine B(1) revealed that these inhibitors exhibit an unprecedented mixed-type inhibition on h-ALR2 with respect to the substrate D,L-glyceraldehyde, in the presence of NADPH at inhibitor concentrations near the IC50 values. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2009.01.020

文献信息

• Synthesis and biological evaluation of 1, 2, 4-oxadiazole derivatives as novel GPR119 agonists
  作者：Suhong Fu、Wei Xiang、Jinying Chen、Liang Ma、Lijuan Chen

  DOI：10.1111/cbdd.12890

  日期：2017.5

  A series of 1,2,4-oxadiazol derivatives have been designed and synthesized and 25 compounds were evaluated their abilities by the assay of cAMP concentration in GPR119-transfected HEK293T cells. All compounds showed acceptable agonistic effects on GPR119. Among these compounds, 4p exhibited the best agonistic effects with the EC50 of 20.6nM, which was comparable to that of positive control GPR119 agonist

  设计并合成了一系列1,2,4-恶二唑衍生物，并通过测定GPR119转染的HEK293T细胞中的cAMP浓度评估了25种化合物的能力。所有化合物对GPR119显示出可接受的激动作用。在这些化合物中，4p表现出最佳的激动作用，EC50为20.6nM，与阳性对照GPR119激动剂GSK1292263相当。这些1,2,4-恶二唑衍生物的激动活性导致建立结构-活性关系。本文受版权保护。版权所有。
• Novel 2-Heteroaryl-Substituted Benzimidazole Derivative
  申请人：Nonoshita Katsumasa

  公开号：US20080070928A1

  公开（公告）日：2008-03-20

  A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided. A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X 1 , X 2 , X 3 and X 4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R 1 represents an aryl, etc.; R 2 represents a hydroxy, etc.; R 3 represents a —C 1-6 alkyl, etc.; R 4 represents a —C 1-6 alkyl, etc.; X 5 represents —O—, etc.; a indicates an integer of 1, 2 or 3; q indicates an integer of from 0 to 2; m indicates an integer of from 0 to 2].

  提供了一种葡萄糖激酶激活剂；提供了糖尿病的治疗和/或预防，或者提供了糖尿病的治疗和/或预防，例如视网膜病变、肾病、神经病、缺血性心脏病、动脉硬化，以及肥胖症的治疗和/或预防。葡萄糖激酶激活剂的特征在于包含通式（I-0）的2-杂环芳基取代苯并咪唑衍生物或其药学上可接受的盐：[在公式中，X表示碳原子或氮原子；X1、X2、X3和X4分别独立地表示碳原子或氮原子；环A表示公式（II）的5-或6-成员含氮芳香杂环：（在公式中，X表示碳原子或氮原子）；R1表示芳基等；R2表示羟基等；R3表示-C1-6烷基等；R4表示-C1-6烷基等；X5表示-O-等；a表示1、2或3的整数；q表示0到2的整数；m表示0到2的整数]。
• Phenylpyrazine derivatives, processes for preparing them, pharmaceutical composition and use
  申请人：SUNTORY LIMITED

  公开号：EP0204172A2

  公开（公告）日：1986-12-10

  Novel phenylpyrazine derivatives of the following general formula: (where R' is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a hydroxyl group; and R2 is a halogen atom, a lower alkyl group, a lower alkoxy group or a hydroxyl group); processes for preparing them, pharmaceutical compositions containing them and their use in the preparation of a medicament for the treatment of thrombotic diseases are described.

  通式如下的新型苯基吡嗪衍生物： (其中，R'是氢原子、卤素原子、低级烷基、低级烷氧基或羟基；R2是卤素原子、低级烷基、低级烷氧基或羟基）；描述了制备它们的工艺、含有它们的药物组合物以及它们在制备治疗血栓性疾病的药物中的用途。
• Compositions for the treatment of pulmonary fibrosis
  申请人：Vectus Biosystems Limited

  公开号：US10919863B2

  公开（公告）日：2021-02-16

  The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

  本发明涉及化合物及其在肺纤维化和/或相关疾病的预防和/或治疗中的用途。
• NOVEL 2-HETEROARYL-SUBSTITUTED BENZIMIDAZOLE DERIVATIVE
  申请人：MSD K.K.

  公开号：EP1702919B1

  公开（公告）日：2012-05-30