Total synthesis and dual PPARα/γ agonist effects of Amorphastilbol and its synthetic derivatives
作者: Taejung KimWoojung LeeKyu Hyuk JeongJung Ho SongSoon-Hye ParkPilju ChoiSu-Nam KimSeokjoon LeeJungyeob Ham
作者单位: 1Natural Medicine Center, Korea Institute of Science and Technology, Gangneung 210-340, Republic of Korea
2Department of Basic Science, Kwandong University College of Medicine, Gangneung 210-701, Republic of Korea
刊名: Bioorganic & Medicinal Chemistry Letters, 2012, Vol.22 (12), pp.4122-4126
来源数据库: Elsevier Journal
DOI: 10.1016/j.bmcl.2012.04.062
关键词: Natural productAmorphastilbolType 2 diabetesDual PPARα/γ agonistsSuzuki–Miyaura cross-coupling
英文摘要: Abstract(#br)Amorphastilbol (APH-1), isolated from a Robinia pseudoacacia var. umbraculifer seed extract, is a biologically interesting natural trans -stilbene compound with dual peroxisome proliferator-activated receptor (PPAR) α/γ agonist activity. After total synthesis of APH-1 and its derivatives by Pd-catalyzed Suzuki–Miyaura cross-coupling of a common ( E )-styryl bromide intermediate and various aromatic trifluoroborate compounds, we biologically evaluated APH-2–APH-12 for PPAR agonist activity. APH-4 and APH-11 were effective PPARα/γ transcriptional activators, compared with APH-1. Therefore, we suggest that APH-4 and APH-11 are novel dual PPARα/γ agonists and are potentially useful for treating type 2 diabetes by enhancing glucose and lipid metabolism.
全文获取路径: Elsevier  (合作)
影响因子:2.338 (2012)

  • diabetes 糖尿病
  • synthetic 合成的
  • coupling 连接
  • synthesis 合成
  • Suzuki 铃木牌摩托车
  • agonist 织肌
  • derivatives 派生物
  • cross 十字
  • effects 海员自身物品
  • product 产物