(E)-3-(8-methoxyquinolin-2-yl)acrylic acid | 91901-29-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: (E)-3-(8-methoxyquinolin-2-yl)acrylic acid
• 英文别名: 3t-(8-methoxy-[2]quinolyl)-acrylic acid；3t-(8-Methoxy-[2]chinolyl)-acrylsaeure；(E)-3-(8-methoxyquinolin-2-yl)prop-2-enoic acid
• CAS: 91901-29-0
• 化学式: C₁₃H₁₁NO₃
• 分子量: 229.235
• InChiKey: LOGDUDLYCLORGI-BQYQJAHWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  59.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (E)-3-(8-methoxyquinolin-2-yl)acrylic acid 在 盐酸 、 乙醇 作用下， 生成 3t-(8-methoxy-[2]quinolyl)-acrylic acid ethyl ester
  参考文献：
  名称：

  Donor finger morbidity in cross-finger flaps

  摘要：

  We reviewed 16 patients who had cross-finger flap procedures carried out between 1991 and 1996 at the West Midlands Regional centre for Plastic and Reconstructive Surgery. We looked specifically at the donor finger morbidity of each patient with a median follow up interval of 43 months.At follow up there were 10 patients with cold intolerance, eight patients with subjective joint stiffness and a documented reduced range of finger joint movement. Skin graft reconstruction of the secondary defect was associated with poor colour match in eight cases (seven hyperpigmented, one hypopigmented) and visible contour deformity in eight cases. There were no clinically significant differences between split skin graft or full thickness skin graft for donor finger reconstruction.Although cross-finger flaps may provide soft tissue cover in a variety of finger pulp injuries, these results show an alarming incidence of donor finger morbidity associated with such procedures. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0020-1383(99)00205-3
• 作为产物：
  描述：

  甲氧甲基喹啉 在 吡啶 、 selenium(IV) oxide 作用下， 以 1,4-二氧六环 为溶剂， 反应 4.0h， 生成 (E)-3-(8-methoxyquinolin-2-yl)acrylic acid
  参考文献：
  名称：

  C-2和C-3取代喹啉的合成及其作为抗HIV-1药物的评价

  摘要：

  据报道许多含有喹啉部分的天然产物和合成衍生物具有各种药理活性。喹啉，例如2-苯乙烯基喹啉和8-羟基喹啉具有广泛的抗HIV-1活性研究，发现主要通过抑制HIV-1整合酶发挥作用。在我们继续努力寻找新的抗HIV-1分子的过程中，合成了31个具有与辅助苯环不同接头的喹啉衍生物，并使用TZM-b1分析评估了其体外抗HIV-1活性。化合物31在TZM-b1细胞系中表现出更高的抗HIV-1 VB59和HIV-1 UG070细胞相关病毒的活性（IC 50与其他衍生工具相比，则为3.35±0.87和2.57±0.71μM）。化合物31还针对无细胞病毒HIV-1 VB59和HIV-1 UG070（IC 50 1.27±0.31和2.88± 1.79μM，TI 42.20和18.61）进行了进一步测试。该先导分子在病毒进入抑制试验和细胞融合试验中也显示出良好的活性，从而确定了其作用方式。通过在活化的外周血单核细胞（PBMC）中针对HIV-1

  DOI：

  10.1016/j.bioorg.2018.07.016

文献信息

• HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
  申请人：Campbell John Emmerson

  公开号：US20130158003A1

  公开（公告）日：2013-06-20

  Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.

  本文提供了杂环芳基化合物、其合成方法、包含该化合物的药物组合物以及使用该化合物的方法。在一种实施例中，本文提供的化合物可用于治疗、预防和/或管理各种疾病，例如中枢神经系统疾病和代谢性疾病，包括但不限于神经系统疾病、精神病、精神分裂症、肥胖症和糖尿病。
• Substituted quinoxalines and quinoxalinones as PDE-10 inhibitors
  申请人：Campbell John Emmerson

  公开号：US08969349B2

  公开（公告）日：2015-03-03

  Provided herein are compounds of formula A-L-B, and pharmaceutically acceptable salts and stereoisomers thereof, wherein A is R1 and R2 together with the carbon atoms to which they are attached form a 1,2-phenylene ring optionally substituted with one or more R11; L is —C(R6)2—C(R6)2—; B is a heteroaromatic group defined herein; and -A1-A2- , A3, R11 and R6 are defined herein. Also disclosed are methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.

  本文提供了A-L-B式化合物及其药学上可接受的盐和立体异构体，其中A为R1和R2，与它们连接的碳原子形成一个可选择地取代一个或多个R11的1,2-苯撑环；L为—C（R6）2—C（R6）2—；B为在本文中定义的杂环芳基；-A1-A2-、A3、R11和R6在本文中定义。还披露了它们的合成方法、包含这些化合物的药物组合物以及它们的使用方法。在一个实施例中，本文提供的化合物可用于治疗、预防和/或管理各种疾病，如中枢神经系统疾病和代谢性疾病，包括但不限于神经系统疾病、精神病、精神分裂症、肥胖症和糖尿病。
• Heteroaryl Compounds and Methods of Use Thereof
  申请人：SUNOVION PHARMACEUTICALS INC.

  公开号：US20150166571A1

  公开（公告）日：2015-06-18

  Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.

  本文提供了杂环芳基化合物、它们的合成方法、包含这些化合物的药物组合物以及它们的使用方法。在一种实施方式中，本文提供的化合物可用于治疗、预防和/或管理各种疾病，例如中枢神经系统疾病和代谢性疾病，包括但不限于神经系统疾病、精神病、精神分裂症、肥胖症和糖尿病等。
• Substituted quinoxalines as PDE-10 inhibitors
  申请人：SUNOVION PHARMACEUTICALS INC.

  公开号：US10562916B2

  公开（公告）日：2020-02-18

  Provided herein are cyclic nucleotide phosphodiesterase inhibitors, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorder.

  本文提供了环核苷酸磷酸二酯酶抑制剂及其药物组合物，可用于治疗中枢神经系统和代谢疾病及紊乱等。
• [EN] HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF<br/>[FR] COMPOSÉS HÉTÉROARYLÉS ET LEURS PROCÉDÉS D'UTILISATION
  申请人：SUNOVION PHARMACEUTICALS INC

  公开号：WO2011150156A3

  公开（公告）日：2012-04-19