The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor.
Bioorganic & Medicinal Chemistry Letters(2011)
摘要
A series of small molecules based on a chemotype identified from our compound collection were synthesized and tested for binding affinity (IC50) at the human Neuropeptide Y Y2 receptor (NPY Y2). Six of the 23 analogs tested possessed an NPY Y2 IC50⩽15nM. One member of this series, JNJ 31020028, is a selective, high affinity, receptor antagonist existing as a racemic mixture. As such a synthetic route to the desired enantiomer was designed starting from commercially available (S)-(+)-mandelic acid.
更多查看译文
关键词
DCM,HOBt,EDCI,BOC,MeOH,K2CO3,Na2CO3,DMF,Et3N,Et2O,HCl,NBS,AIBN,CCl4,DCC,EtOAc,MsCl,NaHCO3,NaOH,Na2SO4,TFA,THF,DIPEA
AI 理解论文
溯源树
样例
![](https://originalfileserver.aminer.cn/sys/aminer/pubs/mrt_preview.jpeg)
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要