Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers.

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Gu SJ, Lee JK, Pae AN, Chung HJ, Rhim H, Han SY, Min SJ, Cho YS

Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers.

Bioorg Med Chem Lett. 2010 May 1;20(9):2705-8. doi: 10.1016/j.bmcl.2010.03.084. Epub 2010 Mar 28.

PubMed ID

20382529 [ View in PubMed

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Abstract

We have synthesized and biologically evaluated 1,4-diazepane derivatives as T-type calcium channel blockers. In this study, we discovered compound 4s, a potential T-type calcium channel blocker with good selectivity over hERG and N-type calcium channels. In addition, it exhibited favorable pharmacokinetic characteristics for further investigation of T-type calcium channel related diseases.

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