首页 | 本学科首页   官方微博 | 高级检索  
     


Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors
Authors:Jung-eun Park  Chiman Song  Keehyun Choi  Taebo Sim  Bongjin Moon  Eun Joo Roh
Affiliation:1. Chemical Kinomics Research Center, Korea Institute of Science and Technology, Wolsong-gil 5, Seongbuk-gu, Seoul, Republic of Korea;2. Department of Chemistry, Sogang University, Baekbeomno 35, Mapogu, Seoul, Republic of Korea
Abstract:A series of 3,4-diarylpyrrolidin-2-one was designed, prepared and evaluated as triple reuptake inhibitors for antidepressant. Most compounds exhibited comparable in vitro efficacy as norepinephrine and dopamine transporter reuptake inhibitors. Especially, 2i showed better potency than GBR-12909 (IC50 = 14 nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 μM–85.6 nM) for three transporters.
Keywords:Triple reuptake inhibitors  Monoamine  Reuptake  Depression  Antidepressant  Serotonin  Dopamine  Norepinephrine  Lactam
本文献已被 ScienceDirect 等数据库收录!
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号