Aryl sulfonamido tetralin inhibitors of the Kv1.5 ion channel

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3063-6. doi: 10.1016/j.bmcl.2009.04.002. Epub 2009 Apr 8.

Abstract

Aryl sulfonamido tetralins based on lead compound 2a were synthesized and evaluated for Kv1.5 inhibitory activity. Several compounds having IC(50) values less then 0.1 microM were identified. Kv1.5 inhibitors have the potential to be atrium-selective agents for the treatment of atrial fibrillation.

MeSH terms

  • Anti-Arrhythmia Agents / chemical synthesis*
  • Anti-Arrhythmia Agents / chemistry
  • Anti-Arrhythmia Agents / pharmacology
  • Humans
  • Kv1.5 Potassium Channel / antagonists & inhibitors*
  • Kv1.5 Potassium Channel / metabolism
  • Potassium Channel Blockers / chemical synthesis*
  • Potassium Channel Blockers / chemistry
  • Potassium Channel Blockers / pharmacology
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology
  • Tetrahydronaphthalenes / chemical synthesis*
  • Tetrahydronaphthalenes / chemistry
  • Tetrahydronaphthalenes / pharmacology

Substances

  • Anti-Arrhythmia Agents
  • Kv1.5 Potassium Channel
  • Potassium Channel Blockers
  • Sulfonamides
  • Tetrahydronaphthalenes