- Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.
Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.
Bioorganic & medicinal chemistry letters (2007-12-28)
Jon J Hangeland, Daniel L Cheney, Todd J Friends, Stephen Swartz, Paul C Levesque, Adam J Rich, Lucy Sun, Terry R Bridal, Leonard P Adam, Diane E Normandin, Natesan Murugesan, William R Ewing
PMID18160281
摘要
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.
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