2-(1-piperazinyl)-4-(1-pyrrolidinyl)quinazoline | 123264-78-8

• 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: 2-(1-piperazinyl)-4-(1-pyrrolidinyl)quinazoline
• 英文别名: 2-Piperazin-1-yl-4-pyrrolidin-1-ylquinazoline
• CAS: 123264-78-8
• 化学式: C₁₆H₂₁N₅
• 分子量: 283.376
• InChiKey: JZVVYIHRXPEKLS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  44.3
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  呋喃甲酰氯 、 2-(1-piperazinyl)-4-(1-pyrrolidinyl)quinazoline 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 以72%的产率得到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
• 作为产物：
  描述：

  1-甲醛哌嗪 、 2-氯-4-(吡咯烷-1-基)喹唑啉 在 盐酸 、 三乙胺 作用下， 生成 2-(1-piperazinyl)-4-(1-pyrrolidinyl)quinazoline
  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.