Peer-reviewed veterinary case report
Synthesis and evaluation of alpha,alpha'-disubstituted phenylacetate derivatives for T-type calcium channel blockers.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2008
- Authors:
- Lee, Hyung Kook et al.
- Affiliation:
- Korea Institute of Science and Technology · South Korea
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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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/18625556/