Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists

Bioorg Med Chem Lett. 1999 Feb 22;9(4):619-22. doi: 10.1016/s0960-894x(99)00040-2.

Abstract

The discovery, synthesis and structure-activity relationships of a series of novel benzofuro[3,2-b]pyridines as non-selective endothelin ET(A)/ET(B) as well as selective ET(B) receptor antagonists are described. The most potent non-selective inhibitor 7s displayed an IC50 of 21 nM and 41 nM for ET(A) and ET(B) receptors, respectively, whereas 7ee merely showed affinity for the ET(B) receptor (IC50 = 3.6 nM).

MeSH terms

  • Animals
  • Endothelin Receptor Antagonists*
  • Endothelin-1 / metabolism
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / metabolism
  • In Vitro Techniques
  • Kidney / drug effects
  • Kidney / metabolism
  • Pyridines / chemistry
  • Pyridines / pharmacology*
  • Rabbits
  • Rats
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • Structure-Activity Relationship
  • Swine

Substances

  • Endothelin Receptor Antagonists
  • Endothelin-1
  • Pyridines
  • Receptor, Endothelin A
  • Receptor, Endothelin B