• Title of article

    Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers

  • Author/Authors

    Hyewhon Rhim، نويسنده , , Yong Sup Lee، نويسنده , , Seong Jun Park، نويسنده , , Bong Young Chung، نويسنده , , Jae Yeol Lee، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2005
  • Pages
    4
  • From page
    283
  • To page
    286
  • Abstract
    We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca2+ channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca2+ channels and N-type Ca2+ channels. Among them, 5b (KYS05044, IC50 = 0.56 ± 0.10 μM) was identified as potent T-type Ca2+ channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI = >100).
  • Keywords
    3 , 4-Dihydroquinazolines , Channel selectivity , blockers , T-type Ca2+ channel , mibefradil
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2005
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    795193