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1-benzyl-3-thioaryl-2-carboxyindoles as potent non-peptide endothelin antagonists

✍ Scribed by Amy M. Bunker; Jeremy J. Edmunds; Kent A. Berryman; Donnelle M. Walker; Michael A. Flynn; Kathy M. Welch; Annette M. Doherty

Book ID: 103983447
Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 242 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(96)00232-6

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✦ Synopsis

Endothelin-1 is a potent vasoconstrictor which is thought to be involved in many human disease states. We have developed a series of indole non-peptide endothelin antagonists which display nanomolar receptor affinity. The representative compound from this series is PD 159433 ( 22), an ETA selective antagonist with an IC50 of 2 nM. The discovery, synthesis and structure-activity relationships of this series of compounds are described.

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