Synthesis and evaluation of alpha,alpha'-disubstituted phenylacetate derivatives for T-type calcium channel blockers.

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Lee HK, Lee YS, Roh EJ, Rhim H, Lee JY, Shin KJ

Synthesis and evaluation of alpha,alpha'-disubstituted phenylacetate derivatives for T-type calcium channel blockers.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4424-7. doi: 10.1016/j.bmcl.2008.06.037. Epub 2008 Jun 14.

PubMed ID

18625556 [ View in PubMed

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Abstract

We have synthesized and evaluated alpha,alpha'-disubstituted phenylacetate derivatives that were designed as T-type calcium channel blockers. Among them, compound 10e (IC(50)=8.17+/-0.48nM) showed the most potent T-type calcium current blocking activity and higher potency than Mibefradil (IC(50)=1.34+/-0.49microM). The PK profile and subtype selectivity over L-type calcium channel were satisfied for further animal assay using disease model.

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