| 1093395-49-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• CAS: 1093395-49-3
• 化学式: C₂₁H₁₉Cl₃N₂O₂
• 分子量: 437.753
• InChiKey: BCARYHYEHDMPCC-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  在 肼 作用下， 以 乙醇 为溶剂， 生成
  参考文献：
  名称：

  Biarylpyrazolyl Oxadiazole as Potent, Selective, Orally Bioavailable Cannabinoid-1 Receptor Antagonists for the Treatment of Obesity

  摘要：

  Since the CB1 cannabinoid receptor antagonist 1 (SR141716, rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. In the present study, biarylpyrazole analogues based on a pyrazole core coupled with 1,3,4-oxadiazole were synthesized and tested for CB1 receptor binding affinity. Thorough SAR studies to optimize pyrazole substituents as well as 1,3,4-oxadiazole ring led to several novel CB1 antagonists with IC50 similar to 1 nM for the CB1 receptor binding. Among these analogues, we identified 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-pyrazol-3-yl)-5-(1-(trifluoromethyl)cyclopropyl)-1,3,4-oxa- diazole 43c as a promising precandidate for the development as an antiobesity agent.

  DOI：

  10.1021/jm800843r