1-(2-furanylcarbonyl)-4-<4-(1-pyrrolidinyl)-2-quinazolinyl>piperazine | 123264-76-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-(2-furanylcarbonyl)-4-<4-(1-pyrrolidinyl)-2-quinazolinyl>piperazine
• 英文别名: 2-[4-(2-Furoyl)-1-piperazinyl]-4-(1-pyrrolidinyl)quinazoline；furan-2-yl-[4-(4-pyrrolidin-1-ylquinazolin-2-yl)piperazin-1-yl]methanone
• CAS: 123264-76-6
• 化学式: C₂₁H₂₃N₅O₂
• 分子量: 377.446
• InChiKey: OPUINEZXNVLKPH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  65.7
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-氯-4-(吡咯烷-1-基)喹唑啉 在 盐酸 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 5.0h， 生成 1-(2-furanylcarbonyl)-4-<4-(1-pyrrolidinyl)-2-quinazolinyl>piperazine
  参考文献：
  名称：

  Atrial natriuretic peptide receptor modulators: effects of disubstituted quinazolines on receptor binding and in vitro biological activity

  摘要：

  Prazosin (25 microM) was found to increase 125I-labeled rat atrial natriuretic peptide ([125I]rANP) receptor binding by 50% (SC50) in bovine adrenal zona glomerulosa membranes. A series of 2,4-disubstituted quinazolines was prepared in order to identify more potent analogues for additional in vitro testing. Compound 7 (N-[3-[[2-(diethyl-amino)-4-quinazolinyl]amino]propyl] guanidine dinitrate) from this series (3 microM) significantly decreased the EC50 for rANP-mediated inhibition of ACTH-stimulated aldosterone synthesis in rat adrenal glomerulosa cells. At a higher concentration (20 microM), compound 7 had no effect on particulate guanylate cyclase from rabbit glomeruli in either the presence or absence of rANP.

  DOI：

  10.1021/jm00163a056

文献信息

• Atrial natriuretic peptide receptor modulators: effects of disubstituted quinazolines on receptor binding and in vitro biological activity
  作者：Melvin J. Yu、Jefferson R. McCowan、Mitchell I. Steinberg、Sally A. Wiest、Virginia L. Wyss、Jong Sin Horng

  DOI：10.1021/jm00163a056

  日期：1990.1

  Prazosin (25 microM) was found to increase 125I-labeled rat atrial natriuretic peptide ([125I]rANP) receptor binding by 50% (SC50) in bovine adrenal zona glomerulosa membranes. A series of 2,4-disubstituted quinazolines was prepared in order to identify more potent analogues for additional in vitro testing. Compound 7 (N-[3-[[2-(diethyl-amino)-4-quinazolinyl]amino]propyl] guanidine dinitrate) from this series (3 microM) significantly decreased the EC50 for rANP-mediated inhibition of ACTH-stimulated aldosterone synthesis in rat adrenal glomerulosa cells. At a higher concentration (20 microM), compound 7 had no effect on particulate guanylate cyclase from rabbit glomeruli in either the presence or absence of rANP.