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ID: ALA1144492
Journal: Bioorg Med Chem
Title: Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Authors: Jo MN, Seo HJ, Kim Y, Seo SH, Rhim H, Cho YS, Cha JH, Koh HY, Choo H, Pae AN.
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 IC(50) value of 1.52 microM, which is comparable to that of mibefradil.
CiteXplore: 17035033