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. 2007 Jan 1;15(1):365-73.
doi: 10.1016/j.bmc.2006.09.051. Epub 2006 Oct 10.

Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives

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Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives

Mi Na Jo et al. Bioorg Med Chem. .

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.

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