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

…, KA Berryman, DM Walker, MA Flynn, KM Welch…

Index: Bunker, Amy M.; Edmunds, Jeremy J.; Berryman, Kent A.; Walker, Donnelle M.; Flynn, Michael A.; Welch, Kathy M.; Doherty, Annette M. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 9 p. 1061 - 1066

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Citation Number: 27

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 ETA selective antagonist, and PD 159020 (37), a non- selective ETA/ETB antagonist. The discovery, synthesis, and structure-activity relationships of this series of compounds are described.