Author/Authors :
Mi Na Jo، نويسنده , , Hee Jeong Seo، نويسنده , , Yoonji Kim، نويسنده , , Seon Hee Seo، نويسنده , , Hyewhon Rhim، نويسنده , , Yong Seo Cho، نويسنده , , Joo Hwan Cha، نويسنده , , Hun Yeong Koh، نويسنده , , Hyunah Choo، نويسنده , , Ae Nim Pae، نويسنده ,
Abstract :
T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pains. Since the withdrawal of mibefradil, a T-type calcium channel blocker, there have been a lot of efforts to develop T-type calcium channel blockers. A small molecule library of dioxoquinazoline carboxamide derivatives containing 155 compounds was designed, synthesized, and biologically evaluated for T-type calcium channel blocking activity. Among those compounds synthesized, the compound 1n shows the most potent T-type calcium current blocking activity with an IC50 value of 1.52 μM, which is comparable to that of mibefradil.
