Facile synthesis and biological evaluation of 3,3-diphenylpropanoyl piperazines as T-type calcium channel blockers.

Article Details

Citation
Copy to clipboard

Choi YH, Baek du J, Seo SH, Lee JK, Pae AN, Cho YS, Min SJ

Facile synthesis and biological evaluation of 3,3-diphenylpropanoyl piperazines as T-type calcium channel blockers.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):215-9. doi: 10.1016/j.bmcl.2010.11.033. Epub 2010 Nov 12.

PubMed ID
21126876 [ View in PubMed
]
Abstract

We have developed a facile synthesis of 3,3-diphenylpropanamides using Meldrum's acid derivatives as amide coupling components. The in vitro biological evaluation of the title compounds led to the identification of compound 1h, which has good inhibitory activity against T-type calcium channel (IC(50) = 0.83 muM).

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
FlunarizineVoltage-dependent T-type calcium channel subunit alpha-1GKd (nM)530N/AN/ADetails
FlunarizineVoltage-dependent T-type calcium channel subunit alpha-1IKd (nM)840N/AN/ADetails
MibefradilVoltage-dependent T-type calcium channel subunit alpha-1GIC 50 (nM)1340N/AN/ADetails