1-BENZYL-3-THIOARYL-2-CARBOXYINDOLES AS POTENT NONPEPTIDE ENDOTHELIN ANTAGONISTS

Authors
BUNKER AM EDMUNDS JJ BERRYMAN KA WALKER DM FLYNN MA WELCH KM DOHERTY AM
Citation
Am. Bunker et al., 1-BENZYL-3-THIOARYL-2-CARBOXYINDOLES AS POTENT NONPEPTIDE ENDOTHELIN ANTAGONISTS, Bioorganic & medicinal chemistry letters, 6(12), 1996, pp. 1367-1370
Citations number
27
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
12
Year of publication
1996
Pages
1367 - 1370
Database
ISI
SICI code
0960-894X(1996)6:12<1367:1APNEA>2.0.ZU;2-C
Abstract
Endothelin-1 is a potent vasoconstrictor which is thought to be involv ed in many human disease states. We have developed a series of indole non-peptide endothelin antagonists which display nanomolar receptor af finity. The representative compound from this series is PD 159433 (22) , an ET(A) selective antagonist with an IC50 of 2 nM. The discovery, s ynthesis and structure-activity relationships of this series of compou nds are described. Copyright (C) 1996 Elsevier Science Ltd