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. doi: 10.1016/j.bmcl.2007.11.103.
Jon J Hangeland  1 ,  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
Affiliations
PMID: 18160281 DOI: 10.1016/j.bmcl.2007.11.103
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.