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]
- 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.
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- 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