7-(4-((1r,4r)-4-((1H-tetrazol-5-yl)methyl)cyclohexyl)phenyl)-N-phenyl-2H-benzo[b][1,4]oxazine-4(3H)-carboxamide | 1245710-42-2

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 7-(4-((1r,4r)-4-((1H-tetrazol-5-yl)methyl)cyclohexyl)phenyl)-N-phenyl-2H-benzo[b][1,4]oxazine-4(3H)-carboxamide
• CAS: 1245710-42-2
• 化学式: C₂₉H₃₀N₆O₂
• 分子量: 494.596
• InChiKey: BDFNWCJWLVVMQD-MEMLXQNLSA-N

反应信息

• 作为产物：
  描述：

  7-(4-((1s,4s)-4-(cyanomethyl)cyclohexyl)phenyl)-N-phenyl-2H-benzo[b][1,4]oxazine-4(3H)-carboxamide 在 叠氮基三甲基硅烷 、 三甲基铝 作用下， 以 甲苯 为溶剂， 反应 48.0h， 以60%的产率得到7-(4-((1r,4r)-4-((1H-tetrazol-5-yl)methyl)cyclohexyl)phenyl)-N-phenyl-2H-benzo[b][1,4]oxazine-4(3H)-carboxamide
  参考文献：
  名称：

  Development of Novel Benzomorpholine Class of Diacylglycerol Acyltransferase I Inhibitors

  摘要：

  Diacylglycerol acyltransferase 1 (DGAT1) presents itself as a potential therapeutic target for obesity and diabetes for its important role in triglyceride biosynthesis. Herein we report the rational design of a novel class of DGAT1 inhibitors featuring a benzomorpholine core (23n). SAR exploration yielded compounds with good potency and selectivity as well as reasonable physical and pharmacokinetic properties. This class of DGAT1 inhibitors was tested in rodent models to evaluate DGAT1 inhibition as a novel approach for the treatment of metabolic diseases. Compound 23n conferred weight loss and a reduction in liver triglycerides when dosed chronically in mice with diet-induced obesity and depleted serum triglycerides following a lipid challenge.

  DOI：

  10.1021/ml400527n