Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.
Article Details
- CitationCopy to clipboard
Hangeland JJ, Cheney DL, Friends TJ, Swartz S, Levesque PC, Rich AJ, Sun L, Bridal TR, Adam LP, Normandin DE, Murugesan N, Ewing WR
Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.
Bioorg Med Chem Lett. 2008 Jan 15;18(2):474-8. Epub 2007 Dec 3.
- PubMed ID
- 18160281 [ View in PubMed]
- Abstract
T-type calcium channel antagonists were designed using a protocol involving the program SPROUT and constrained by a ComFA-based pharmacophore model. Scaffolds generated by SPROUT were evaluated based on their ability to be translated into structures that were synthetically tractable. From this exercise, a novel series of potent and selective T-type channel antagonists containing a biaryl sulfonamide core were discovered.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Mibefradil Voltage-dependent T-type calcium channel subunit alpha-1H IC 50 (nM) 130 N/A N/A Details