Isoindolines: A New Series of Potent and Selective Endothelin-A Receptor Antagonists.

Abstract 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.