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

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.

T-type calcium channel antagonists were designed using a protocol involving the program SPROUT constrained by a ComFA-based pharmacophore model. From this exercise, a novel series of potent and selective T-type channel antagonists containing a biaryl sulfonamide core were discovered.Figure optionsDownload as PowerPoint slide