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

Bioorganic & Medicinal Chemistry Letters
2005.0

Abstract

We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca(2+) channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca(2+) channels and N-type Ca(2+) channels. Among them, 5b (KYS05044, IC(50)=0.56+/-0.10 microM) was identified as potent T-type Ca(2+) channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI=>100).

DOI： 10.1016/j.bmcl.2004.10.078

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