N-(5-phenylpyrazin-2-yl)spiro[isochroman-1,4''-piperidine]-1''-carboxamide | 1175705-99-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: N-(5-phenylpyrazin-2-yl)spiro[isochroman-1,4''-piperidine]-1''-carboxamide
• 英文别名: N-(5-phenylpyrazin-2-yl)spiro[3,4-dihydroisochromene-1,4'-piperidine]-1'-carboxamide
• CAS: 1175705-99-3
• 化学式: C₂₄H₂₄N₄O₂
• 分子量: 400.48
• InChiKey: TUMSRTFIRFTRCG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  30
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  67.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  (5-苯基吡嗪-2-基)氨基甲酸苯酯 、 螺[异苯并二氢吡喃-1,4’-哌啶] 生成 N-(5-phenylpyrazin-2-yl)spiro[isochroman-1,4''-piperidine]-1''-carboxamide
  参考文献：
  名称：

  Aryl urea derivatives of spiropiperidines as NPY Y5 receptor antagonists

  摘要：

  Continuing medicinal chemistry studies to identify spiropiperidine-derived NPY Y5 receptor antagonists are described. Aryl urea derivatives of a variety of spiropiperidines were tested for their NPY Y5 receptor binding affinities. Of the spiropiperidines so far examined, spiro[3-oxoisobenzofurane-1(3H),4 '-piperidine] was a useful scaffold for producing orally active NPY Y5 receptor antagonists. Oral administration of 5c significantly inhibited the Y5 agonist-induced food intake in rats with a minimum effective dose of 3 mg/kg. In addition, this compound was efficacious in decreasing body weight in diet-induced obese mice. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.05.013