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. 2008 Jan 15;18(2):474-8.
doi: 10.1016/j.bmcl.2007.11.103. Epub 2007 Dec 3.

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

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

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

Jon J Hangeland et al. Bioorg Med Chem Lett. .

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.

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