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

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

Affiliation

  • 1 Bristol-Myers Squibb R& D, Princeton, NJ 08543-5400, USA. jon.hangeland@bms.com
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.

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