2,8-二甲基-1,5-萘啶 | 764717-59-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 2,8-二甲基-1,5-萘啶
• 英文名称: 2,8-dimethyl[1,5]naphthyridine
• 英文别名: 2,8-Dimethyl-1,5-naphthyridine
• CAS: 764717-59-1
• 化学式: C₁₀H₁₀N₂
• mdl: MFCD09038140
• 分子量: 158.203
• InChiKey: OWLRUQWOUYITHU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2,8-二甲基-1,5-萘啶 在 溴 、 双(三甲基硅烷基)氨基钾 作用下， 以 四氢呋喃 、 1,4-二氧六环 为溶剂， 反应 1.0h， 生成
  参考文献：
  名称：

  Discovery and structure activity relationship of the first potent cryptosporidium FIKK kinase inhibitor

  摘要：

  FIKKs are parasite -specific protein kinases with distinctive sequence motifs and their biological roles have not been completely elucidated. Here, we report the first potent Cryptosporidium FIKK (CpFIKK) inhibitor. We identified 4b as a potent (IC50 = 0.2 nM) inhibitor of CpFIKK catalytic activity. In addition, we identified both CpCDPK1 selective as well as dually acting CpFIKK-CDPK1 inhibitors from the same structural class of compounds. We evaluated these CpFIKK inhibitors for inhibition of parasite growth in vitro. The observed effects on parasite growth did not correlate with CpFIKK inhibition, suggesting that CpFIKK may not be involved in parasite growth. (C) 2017 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2017.01.036
• 作为产物：
  描述：

  3-氨基-4-甲基吡啶 、 乙醛 在 盐酸 作用下， 反应 1.0h， 以16%的产率得到2,8-二甲基-1,5-萘啶
  参考文献：
  名称：

  1，5-萘啶衍生物的鉴定为一系列新的有效和选择性的I型TGF-β受体抑制剂。

  摘要：

  筛选命中1的优化导致鉴定了新型1,5-萘啶氨基噻唑和吡唑衍生物，它们是转化生长因子βI型受体ALK5的有效抑制剂。分别以IC50 = 6和4 nM抑制ALK5自磷酸化的化合物15和19在结合和细胞分析中均显示出强大的活性，并显示出超过p38促分裂原活化蛋白激酶的选择性。描述了与人ALK5结合的19的X射线晶体结构，证实了对接研究提出的结合模式。

  DOI：

  10.1021/jm0400247

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。
• 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。
• Organic light-emitting device
  申请人：SAMSUNG DISPLAY CO., LTD.

  公开号：US10312449B2

  公开（公告）日：2019-06-04

  An organic light-emitting device including a first electrode, a second electrode, and an organic layer between the first electrode and the second electrode and including an emission layer; wherein the organic layer includes a host first compound represented by Formula 1 and a fluorescent dopant second compound represented by Formula 2: When the compound represented by Formula 1 includes a condensed cyclic substituent and the compound represented by Formula 2 includes a condensed cyclic core, the organic light-emitting device may have improved thermal stability, a lower driving voltage, and higher efficiency.

  一种有机发光器件，包括第一电极、第二电极以及位于第一电极和第二电极之间并包括发射层的有机层；其中有机层包括由式 1 表示的宿主第一化合物和由式 2 表示的荧光掺杂剂第二化合物： 当式 1 所代表的化合物包括缩合环取代基和式 2 所代表的化合物包括缩合环核心时，有机发光器件可能具有更好的热稳定性、更低的驱动电压和更高的效率。
• 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。
• US20140256717A1
  申请人：——

  公开号：US20140256717A1

  公开（公告）日：2014-09-11