N-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamide

• 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: N-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamide
• 英文别名: N-benzyl-4-hydroxy-2-oxo-1H-quinoline-3-carboxamide
• 化学式: C₁₇H₁₄N₂O₃
• mdl: MFCD00572677
• 分子量: 294.3
• InChiKey: WKAZEVUZAKRWHB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  78.4
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• INHIBITORS OF UNDECAPRENYL PYROPHOSPHATE SYNTHASE
  申请人：Hurley Timothy Brian

  公开号：US20090325948A1

  公开（公告）日：2009-12-31

  The present invention relates to compounds that are selective and/or potent inhibitors of UPPS. In addition to compounds which inhibit UPPS, the invention also provides pharmaceutical compositions comprising these compounds and methods of using these compounds for treating bacterial disease, such as bacterial infection.

  本发明涉及选择性和/或有效抑制UPPS的化合物。除了抑制UPPS的化合物外，本发明还提供包含这些化合物的药物组合物以及使用这些化合物治疗细菌性疾病，如细菌感染的方法。
• REPORTER SYSTEM FOR HIGH THROUGHPUT SCREENING OF COMPOUNDS AND USES THEREOF
  申请人：RATAN Rajiv

  公开号：US20130005666A1

  公开（公告）日：2013-01-03

  The NF-E2-related factor 2 (Nrf2) is a key transcriptional regulator of antioxidant defense and detoxification. To directly monitor stabilization of Nrf2 we fused its Neh2 domain, responsible for the interaction with its nucleocytoplasmic regulator, Keap1, to firefly luciferase (Neh2-luciferase). It is shown herein that Neh2 domain is sufficient for recognition, ubiquitination and proteasomal degradation of Neh2-luciferase fusion protein. The novel Neh2-luc reporter system allows direct monitoring of the adaptive response to redox stress and classification of drugs based on the time-course of reporter activation. The novel reporter was used to screen a library of compounds to identify activators of Nrf2. The most robust and yet non toxic Nrf2 activators found—nordihydroguaiaretic acid, fisetin, and gedunin-induced astrocyte-dependent neuroprotection from oxidative stress via an Nrf2-dependent mechanism.
• US9200046B2
  申请人：——

  公开号：US9200046B2

  公开（公告）日：2015-12-01