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

JJ Hangeland, DL Cheney, TJ Friends, S Swartz…

Index: Hangeland, Jon J.; Cheney, Daniel L.; Friends, Todd J.; Swartz, Stephen; Levesque, Paul C.; Rich, Adam J.; Sun, Lucy; Bridal, Terry R.; Adam, Leonard P.; Normandin, Diane E.; Murugesan, Natesan; Ewing, William R. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 2 p. 474 - 478

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Citation Number: 16

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.