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

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Rhim H, Lee YS, Park SJ, Chung BY, Lee JY

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

Bioorg Med Chem Lett. 2005 Jan 17;15(2):283-6.

PubMed ID

15603940 [ View in PubMed

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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).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Mibefradil	Voltage-dependent T-type calcium channel subunit alpha-1G	IC 50 (nM)	1340	N/A	N/A	Details