1,3-DIARYL-2-CARBOXYINDOLES AS POTENT NON-PEPTIDE ENDOTHELIN ANTAGONISTS

Abstract Endothelin-1 is a potent vasoconstrictor that is thought to be involved in many human disease states. We have developed a series of indole non-peptide endothelin antagonists including PD 159110 ( 31 ), an ET A selective antagonist, and PD 159020 ( 37 ), a non-selective ET A /ET B antagonist. The discovery, synthesis, and structure-activity relationships of this series of compounds are described.