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. Epub 2007 Dec 3.

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.

MeSH terms

  • Animals
  • Calcium Channel Blockers / chemistry*
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, T-Type / drug effects*
  • Crystallography, X-Ray
  • Drug Design
  • In Vitro Techniques
  • Patch-Clamp Techniques
  • Structure-Activity Relationship
  • Sulfonamides / chemistry*
  • Sulfonamides / pharmacology*

Substances

  • Calcium Channel Blockers
  • Calcium Channels, T-Type
  • Sulfonamides