Design, syntheses, and SAR of 2,8-diazaspiro[4.5]decanones as T-type calcium channel antagonists.

Article Details

Citation

Fritch PC, Krajewski J

Design, syntheses, and SAR of 2,8-diazaspiro[4.5]decanones as T-type calcium channel antagonists.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6375-8. doi: 10.1016/j.bmcl.2010.09.098. Epub 2010 Sep 19.

PubMed ID
20934333 [ View in PubMed
]
Abstract

It was hypothesized that an appropriately substituted 2,8-diazaspiro[4.5]decan-1-one could effectively approximate a 5-feature T-type pharmacophore model published in the literature. Compounds were designed and synthesized to test our hypothesis and were found to be potent T-type calcium channel inhibitors with modest selectivity over L-type calcium channels. The synthesis and SAR of the series is described.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MibefradilVoltage-dependent T-type calcium channel subunit alpha-1HIC 50 (nM)32N/AN/ADetails