Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat
作者: Thuy-Anh TranYoung-Jun ShinBryan KramerJuyi ChoiNing ZouPureza VallarPeter MartensP. Douglas BoatmanJohn W. AdamsJuan RamirezYunqing ShiMichael MorganDavid J. UnettSteve ChangHsin-Hui ShuShiu-Feng TungGraeme Semple
作者单位: 1Arena Pharmaceuticals, 6154, Nancy Ridge Drive, San Diego, CA 92121, USA
刊名: Bioorganic & Medicinal Chemistry Letters, 2015, Vol.25 (5), pp.1030-1035
来源数据库: Elsevier Journal
DOI: 10.1016/j.bmcl.2015.01.024
关键词: ProstacyclinIP receptor agonistGPCRPAH
原始语种摘要: Abstract(#br)The design and synthesis of two closely related series of prostacyclin receptor agonist compounds that showed excellent human IP receptor potency and efficacy is described. Compounds from this series showed in vivo activity after SC dosing in the monocrotaline model of PAH in rat.
全文获取路径: Elsevier  (合作)
影响因子:2.338 (2012)

  • prostacyclin 环前列腺素
  • receptor 接受体
  • potent 强大的
  • activity 活度
  • agonist 织肌
  • PAH Pitch Attitude Hold
  • series