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

โœ 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
103983400
Publisher
Elsevier Science
Year
1996
Tongue
English
Weight
311 KB
Volume
6
Category
Article
ISSN
0960-894X

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โœฆ Synopsis

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.

๐Ÿ“œ SIMILAR VOLUMES

1-benzyl-3-thioaryl-2-carboxyindoles as
1-benzyl-3-thioaryl-2-carboxyindoles as potent non-peptide endothelin antagonists
โœ Amy M. Bunker; Jeremy J. Edmunds; Kent A. Berryman; Donnelle M. Walker; Michael ๐Ÿ“‚ Article ๐Ÿ“… 1996 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 242 KB

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