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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
Bristol-Myers Squibb R& D
NJ 08543-5400
Published in:
Bioorg. Med. Chem. Lett.
2008, 18(2), pp 474-478

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.
graphical abstract