Isoindolines: a new series of potent and selective endothelin-A receptor antagonists

Bioorg Med Chem Lett. 2001 Jul 9;11(13):1737-40. doi: 10.1016/s0960-894x(01)00273-6.


1,3-Disubstituted isoindolines have been discovered as a new class of potent functional ET(A) selective receptor antagonists through pharmacophore analysis of existing nonpeptide endothelin antagonists. The structure-activity relationships for both the trans and the cis series of isoindolines are discussed.

MeSH terms

  • Endothelin Receptor Antagonists*
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Receptor, Endothelin A
  • Receptors, Endothelin / chemistry


  • Endothelin Receptor Antagonists
  • Indoles
  • Receptor, Endothelin A
  • Receptors, Endothelin