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.