3-acetyl-1-ethyl-7-methyl-4-oxo-1,4-dihydroquinoline | 67503-75-7

• 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: 3-acetyl-1-ethyl-7-methyl-4-oxo-1,4-dihydroquinoline
• 英文别名: 3-Acetyl-1-ethyl-7-methylquinolin-4-one
• CAS: 67503-75-7
• 化学式: C₁₄H₁₅NO₂
• 分子量: 229.279
• InChiKey: OWRJCCIAQWYSCF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-acetyl-1-ethyl-7-methyl-4-oxo-1,4-dihydroquinoline 在 PEG-100 、 selenium(IV) oxide 、 硫酸 、 盐酸羟胺 、 sodium acetate 、 potassium carbonate 作用下， 以 吡啶 、 乙醇 、 丙酮 为溶剂， 反应 11.0h， 生成 (E)-ethyl 2-(1-ethyl-7-methyl-1,4-dihydro-4-oxoquinolin-3-yl)-2-methoxyimino acetate
  参考文献：
  名称：

  Shridhar, D. R.; Ram, Bhagat; Krishna, R. R., Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1986, vol. 25, p. 76 - 80

  摘要：

  DOI：

文献信息

• Compounds for proteasome enzyme inhibition
  申请人：Proteolix, Inc.

  公开号：EP2030981A1

  公开（公告）日：2009-03-04

  Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-termmal nucleophile (Nin) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by she compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

  包括含杂原子的三元环的肽基化合物能有效地、选择性地抑制 N-三卤代亲核物（Nin）水解酶的特定活性。具有多种活性的 Ntn 的活性可受到所述化合物的不同抑制。例如，本发明化合物可选择性地抑制 20S 蛋白酶体的糜蛋白酶样活性。肽基化合物包括环氧化物或氮丙啶，以及 N 端的官能化。除其他治疗作用外，肽基化合物还具有抗炎和抑制细胞增殖的作用。
• Composition for proteasome inhibition
  申请人：Proteolix, Inc.

  公开号：EP2260835A2

  公开（公告）日：2010-12-15

  Compositions comprising one or more practically insoluble proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin, substantially increase the solubility of these proteasome inhibitors and facilitate their administration. Such compositions optionally comprise a buffer. Methods of treatment using such compositions are also disclosed:

  由一种或多种几乎不溶解的蛋白酶体抑制剂和环糊精（特别是取代的环糊精）组成的组合物，可大大提高这些蛋白酶体抑制剂的溶解度，便于给药。此类组合物可选择包含缓冲剂。还公开了使用这种组合物进行治疗的方法：
• SHRIDHAR D. R.; RAM BHAGAT; KRISHNA R. R.; NARAYANA V. LAKSHMI, INDIAN J. CHEM., 25,(1986) N 1, 76-80
  作者：SHRIDHAR D. R.、 RAM BHAGAT、 KRISHNA R. R.、 NARAYANA V. LAKSHMI

  DOI：——

  日期：——
• Compounds For Enzyme Inhibition
  申请人：Smyth S. Mark

  公开号：US20080090785A1

  公开（公告）日：2008-04-17

  Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
• US7737112B2
  申请人：——

  公开号：US7737112B2

  公开（公告）日：2010-06-15