6-hydroxy-4-phenyl-2(1H)-quinolinone | 1402932-06-2

• 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: 6-hydroxy-4-phenyl-2(1H)-quinolinone
• 英文别名: 6-hydroxy-4-phenyl-1H-quinolin-2-one
• CAS: 1402932-06-2
• 化学式: C₁₅H₁₁NO₂
• 分子量: 237.258
• InChiKey: VVILAGDCZXAKHV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  6-methoxy-4-phenylquinolin-2(1H)-one 在 吡啶 作用下， 反应 0.33h， 以92%的产率得到6-hydroxy-4-phenyl-2(1H)-quinolinone
  参考文献：
  名称：

  Synthesis and Evaluation of 4-Aryl-2(1H)-quinolinones as Potent Amyloid β Fibrillogenesis Inhibitors

  摘要：

  4-Aryl-2(1H)-quinolinones were synthesized and evaluated in vitro as inhibitors of A beta(1-42) fibrillogenesis using a thioflavin T fluorescence method. The most potent anti-aggregating molecules (4b and 5c) were found among the derivatives bearing OH and/or OMe groups at C-4' (R-4) and/or C-6 (R-2) of the 4-aryl-2(1H)-quinolinone moiety. Furthermore, the derivative bearing 4'-F substituent (4f) proved to be a very active inhibitor.

  DOI：

  10.3987/com-12-12506

文献信息

• [EN] METHODS AND COMPOSITIONS FOR INHIBITION OF BROMODOMAIN-CONTAINING PROTEINS<br/>[FR] PROCÉDÉS ET COMPOSITIONS POUR L'INHIBITION DE PROTÉINES CONTENANT UN BROMODOMAINE
  申请人：CONVERGENE LLC

  公开号：WO2014159837A1

  公开（公告）日：2014-10-02

  The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

  本发明涉及结合并调节含溴结构域蛋白活性的化合物，以及制备这些化合物的方法、含有这些化合物的药物组合物，以及利用这些化合物治疗各种疾病和疾病的方法。
• QUINOLINE TACHYKININ RECEPTOR ANTAGONISTS
  申请人：Merck & Co., Inc.

  公开号：EP1819342A1

  公开（公告）日：2007-08-22
• EP1819342A4
  申请人：——

  公开号：EP1819342A4

  公开（公告）日：2008-12-17
• [EN] QUINOLINE TACHYKININ RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DE RÉCEPTEURS DE TACHYKININE DE TYPE QUINOLINE
  申请人：MERCK & CO INC

  公开号：WO2006060390A1

  公开（公告）日：2006-06-08

  [EN] The present invention is directed to certain quinoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
  [FR] La présente invention concerne des dérivés de quinoline pouvant être employés en tant qu'antagonistes de récepteurs de neurokinine-1 (NK-1), et en tant qu'inhibiteurs de la tachykinine et en particulier de la substance P. La présente invention concerne également les formules pharmaceutiques comprenant ces composés au titre de principes actifs, ainsi que l'emploi desdits composés et de leurs formules dans le traitement de certains troubles, dont les vomissements, l'incontinence urinaire, la dépression et l'anxiété.
• Synthesis and Evaluation of 4-Aryl-2(1H)-quinolinones as Potent Amyloid β Fibrillogenesis Inhibitors
  作者：Masayoshi Tsubuki、Yoko Shimokawa、Masamichi Nakakoshi、Setsu Saito、Hideharu Suzuki、Yuusaku Yokoyama、Akihito Ishigami、Hideo Nishioka

  DOI：10.3987/com-12-12506

  日期：——

  4-Aryl-2(1H)-quinolinones were synthesized and evaluated in vitro as inhibitors of A beta(1-42) fibrillogenesis using a thioflavin T fluorescence method. The most potent anti-aggregating molecules (4b and 5c) were found among the derivatives bearing OH and/or OMe groups at C-4' (R-4) and/or C-6 (R-2) of the 4-aryl-2(1H)-quinolinone moiety. Furthermore, the derivative bearing 4'-F substituent (4f) proved to be a very active inhibitor.