Bioorganic & Medicinal Chemistry Letters 2008-01-15

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

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

文献索引：Bioorg. Med. Chem. Lett. 18(2) , 474-8, (2008)

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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.