Design, syntheses, and SAR of 2,8-diazaspiro[4.5]decanones as T-type calcium channel antagonists.
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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.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Mibefradil Voltage-dependent T-type calcium channel subunit alpha-1H IC 50 (nM) 32 N/A N/A Details