1-(1H-imidazole-4-yl)pentan-3-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-(1H-imidazole-4-yl)pentan-3-one
• 英文别名: 1-(1H-imidazol-5-yl)pentan-3-one
• 化学式: C₈H₁₂N₂O
• 分子量: 152.196
• InChiKey: WRVTUJKMVZLSEA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  11
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  45.8
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4,4'-二羟基二苯甲酮 、 1-(1H-imidazole-4-yl)pentan-3-one 在 四氯化钛 、 锌 作用下， 以 四氢呋喃 为溶剂， 以11%的产率得到4,4'-(2-ethyl-4-(1H-imidazole-4-yl)but-1-ene-1,1-diyl)diphenol
  参考文献：
  名称：

  Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer

  摘要：

  DOI：

  10.1016/j.ejmech.2021.113733
• 作为产物：
  描述：

  (E)-1-(1H-imidazole-4-yl)pent-1-en-3-one 在 溶剂黄146 、 锌 作用下， 以 水 为溶剂， 反应 3.0h， 以43%的产率得到1-(1H-imidazole-4-yl)pentan-3-one
  参考文献：
  名称：

  Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer

  摘要：

  DOI：

  10.1016/j.ejmech.2021.113733

文献信息

• N-TERMINALLY MODIFIED GLP-1 RECEPTOR MODULATORS
  申请人：Ewing R. William

  公开号：US20080045461A1

  公开（公告）日：2008-02-21

  The subject matter described herein provides novel human glucagon-like peptide-1 (GLP-1) receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. The described compounds include chemically modified peptides that may stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The disclosed and claimed peptides show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

  本文所述主题提供了新颖的人类胰高血糖素样肽-1（GLP-1）受体调节剂，其生物活性类似或优于天然GLP-1肽，因此可用于治疗或预防与GLP活性相关的疾病或疾病。所述化合物包括化学修饰的肽，可以刺激2型糖尿病患者的胰岛素分泌，但也产生其他有益的胰岛素促分泌反应。这些合成肽GLP-1受体调节剂表现出对蛋白酶解的稳定性增加，使它们成为口服或静脉注射的理想治疗候选药物。所披露和声称的肽显示出理想的药代动力学特性和糖尿病疗效模型的理想效力。
• N-terminally modified GLP-1 receptor modulators
  申请人：Ewing R. William

  公开号：US20070021346A1

  公开（公告）日：2007-01-25

  The subject matter described herein provides novel human glucagon-like peptide-1 (GLP-1) receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. The described compounds include chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The disclosed and claimed peptides show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

  本文所描述的主题提供了一种新颖的人类胰高血糖素样肽-1（GLP-1）受体调节剂，其生物活性类似或优于天然GLP-1肽，因此可用于治疗或预防与GLP活性相关的疾病或障碍。所描述的化合物包括化学修饰的肽，不仅能够刺激II型糖尿病患者的胰岛素分泌，还产生其他有益的胰岛素促进反应。这些合成肽GLP-1受体调节剂表现出对蛋白酶水解的稳定性增加，使它们成为口服或静脉注射的理想治疗候选药物。所披露和要求的肽具有理想的药代动力学特性和糖尿病疗效模型中的理想效力。
• Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer
  作者：Jessica Caciolla、Silvia Martini、Angelo Spinello、Matic Pavlin、Eleonora Turrini、Federica Simonelli、Federica Belluti、Angela Rampa、Alessandra Bisi、Carmela Fimognari、Nadia Zaffaroni、Silvia Gobbi、Alessandra Magistrato

  DOI：10.1016/j.ejmech.2021.113733

  日期：2021.11