1,3-Diaryl-2-carboxyindoles as potent non-peptide endothelin antagonists

Article abstract of DOI:10.1016/0960-894X(96)00170-9

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), and 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.