Bis-sulfonamides as endothelin receptor antagonists

Bioorg Med Chem Lett. 2003 Mar 10;13(5):951-4. doi: 10.1016/s0960-894x(02)01083-1.

Abstract

Modification of the structure of bosentan 1, the first marketed endothelin receptor antagonist (Tracleer), by introduction of a second sulfonamide function at the alkoxy side chain, led to bis-sulfonamides 2. This allowed to prepare dual ET(A)/ET(B) as well as ET(B) receptor selective antagonists, which could serve as tools to investigate the pharmacological consequences of selective ET(B) receptor blockade.

MeSH terms

  • Animals
  • Aorta / drug effects
  • Aorta / physiology
  • CHO Cells
  • Cricetinae
  • Endothelin Receptor Antagonists*
  • Humans
  • Inhibitory Concentration 50
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / physiology
  • Rats
  • Receptors, Endothelin / metabolism
  • Structure-Activity Relationship
  • Sulfonamides / chemistry*
  • Sulfonamides / pharmacology*
  • Vasoconstriction / drug effects

Substances

  • Endothelin Receptor Antagonists
  • Receptors, Endothelin
  • Sulfonamides