Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.

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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

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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